Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
46780481 107504 20 None -6 15 Human 8.9 pAC50 = 8.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 107504 20 None -6 15 Human 8.9 pAC50 = 8.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 107504 20 None -6 15 Human 8.9 pAC50 = 8.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 107504 20 None -6 15 Human 8.9 pAC50 = 8.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
3151 1450 97 None -1905 24 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 1450 97 None -1905 24 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 1450 97 None -1905 24 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 1450 97 None -1905 24 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 1450 97 None -1905 24 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
216239 23763 118 None -5 11 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1200485 23763 118 None -5 11 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1336 23763 118 None -5 11 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
2176 49615 81 None - 1 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 6 1 8 2.6 CCOC(=O)OC(C)OC1=C(C(=O)Nc2ccccn2)N(C)S(=O)(=O)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1566249 49615 81 None - 1 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 6 1 8 2.6 CCOC(=O)OC(C)OC1=C(C(=O)Nc2ccccn2)N(C)S(=O)(=O)c2ccccc21 10.1038/s41467-023-40064-9
72106 78163 60 None -3 3 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 6 3.3 O=C(OCCN1CCOCC1)c1cccnc1Nc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL2105059 78163 60 None -3 3 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 6 3.3 O=C(OCCN1CCOCC1)c1cccnc1Nc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
45138674 16614 50 None -5 6 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1241951 16614 50 None -5 6 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
439280 119993 107 None -25 9 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1038/s41467-023-40064-9
6971044 119993 107 None -25 9 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL350221 119993 107 None -25 9 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1038/s41467-023-40064-9
432824 78235 13 None -1 4 Human 6.0 pAC50 = 6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 273 2 0 2 3.5 CC(C)N1CCOC(c2cccc(C(F)(F)F)c2)C1 10.1038/s41467-023-40064-9
CHEMBL2106996 78235 13 None -1 4 Human 6.0 pAC50 = 6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 273 2 0 2 3.5 CC(C)N1CCOC(c2cccc(C(F)(F)F)c2)C1 10.1038/s41467-023-40064-9
242 469 124 None -33 33 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 469 124 None -33 33 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 469 124 None -33 33 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 469 124 None -33 33 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 469 124 None -33 33 Human 7.0 pAC50 = 7.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
123606 351 70 None -199 6 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
128 351 70 None -199 6 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
7110 351 70 None -199 6 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
CHEMBL1505 351 70 None -199 6 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
DB00918 351 70 None -199 6 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
5994 4609 88 None -3 10 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
CHEMBL103 4609 88 None -3 10 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
2335 11816 22 None -81 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11816 22 None -81 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11816 22 None -81 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11816 22 None -81 34 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
3149 12582 15 None -30 26 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12582 15 None -30 26 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
56959 31526 103 None -7 9 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1404 31526 103 None -7 9 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1526084 31526 103 None -7 9 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
4034 55792 55 None -8 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55792 55 None -8 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
71398 106412 44 None -1548 14 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL313972 106412 44 None -1548 14 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
180 400 56 None -398 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 400 56 None -398 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 400 56 None -398 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 400 56 None -398 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 400 56 None -398 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
1890 2739 49 None -2 24 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2739 49 None -2 24 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2739 49 None -2 24 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2739 49 None -2 24 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2739 49 None -2 24 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
3316 31730 71 None 17 4 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 221 7 1 2 2.7 CCCCCCOc1ccccc1C(N)=O 10.1038/s41467-023-40064-9
CHEMBL1405973 31730 71 None 17 4 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 221 7 1 2 2.7 CCCCCCOc1ccccc1C(N)=O 10.1038/s41467-023-40064-9
4993 122331 110 None -5 5 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 2 2 4 2.5 CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL36 122331 110 None -5 5 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 2 2 4 2.5 CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
441074 19382 82 None 1 11 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL1294 19382 82 None 1 11 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
3658 4076 53 None -141 18 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 4076 53 None -141 18 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 4076 53 None -141 18 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 4076 53 None -141 18 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 4076 53 None -141 18 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
191 402 98 None -3 36 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 402 98 None -3 36 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 402 98 None -3 36 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 402 98 None -3 36 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 402 98 None -3 36 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
1613 2333 53 None -5 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2333 53 None -5 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2333 53 None -5 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2333 53 None -5 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2333 53 None -5 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4640 78237 30 None 1 11 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2107011 78237 30 None 1 11 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
3158 56237 27 None -323 28 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56237 27 None -323 28 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
4011 82379 49 None -75 26 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82379 49 None -75 26 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
2520 203985 70 None -1 20 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1280 203985 70 None -1 20 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL6966 203985 70 None -1 20 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
5906 14463 23 None 1 4 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 167 2 3 3 0.8 C[C@H](N)[C@H](O)c1cccc(O)c1 10.1038/s41467-023-40064-9
CHEMBL1201319 14463 23 None 1 4 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 167 2 3 3 0.8 C[C@H](N)[C@H](O)c1cccc(O)c1 10.1038/s41467-023-40064-9
72093 35031 9 None -2 28 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35031 9 None -2 28 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35031 9 None -2 28 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
4746 204868 31 None -10 19 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 204868 31 None -10 19 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 204868 31 None -10 19 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
1012 26 86 None -7079 4 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1038/s41467-023-40064-9
1013 26 86 None -7079 4 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1038/s41467-023-40064-9
1057 26 86 None -7079 4 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1038/s41467-023-40064-9
5757 26 86 None -7079 4 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1038/s41467-023-40064-9
CHEMBL135 26 86 None -7079 4 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1038/s41467-023-40064-9
DB00783 26 86 None -7079 4 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 272 0 2 2 3.6 Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2O)C 10.1038/s41467-023-40064-9
1224 1420 83 None -707 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1420 83 None -707 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1420 83 None -707 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1420 83 None -707 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1420 83 None -707 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1420 83 None -707 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
202 1496 77 None -8 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1496 77 None -8 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1496 77 None -8 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1496 77 None -8 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1496 77 None -8 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
2419 3437 84 None -25703 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
5152 3437 84 None -25703 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
559 3437 84 None -25703 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL1263 3437 84 None -25703 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
DB00938 3437 84 None -25703 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
5077 3552 79 None -457 13 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
7552 3552 79 None -457 13 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
9913767 3552 79 None -457 13 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
CHEMBL238804 3552 79 None -457 13 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
DB11362 3552 79 None -457 13 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
2855 4101 104 None -6025 12 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
3322 4101 104 None -6025 12 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
5717 4101 104 None -6025 12 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
CHEMBL603 4101 104 None -6025 12 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
DB00549 4101 104 None -6025 12 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
5029 15513 92 None -6 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 359 8 1 5 3.0 COCCCOc1ccnc(C[S+]([O-])c2nc3ccccc3[nH]2)c1C 10.1038/s41467-023-40064-9
CHEMBL1219 15513 92 None -6 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 359 8 1 5 3.0 COCCCOc1ccnc(C[S+]([O-])c2nc3ccccc3[nH]2)c1C 10.1038/s41467-023-40064-9
2162 41484 100 None -6 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41484 100 None -6 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
47510 172522 39 None -7 3 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 220 1 3 2 1.4 CN=C(N)NC(=O)Nc1c(C)cccc1C 10.1038/s41467-023-40064-9
CHEMBL448416 172522 39 None -7 3 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 220 1 3 2 1.4 CN=C(N)NC(=O)Nc1c(C)cccc1C 10.1038/s41467-023-40064-9
22323 15267 32 None -6 11 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9571037 15267 32 None -6 11 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1213553 15267 32 None -6 11 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
2895 203569 41 None -60 15 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL669 203569 41 None -60 15 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
2713 205248 82 None -1 27 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 205248 82 None -1 27 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 205248 82 None -1 27 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 205248 82 None -1 27 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 205248 82 None -1 27 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 205248 82 None -1 27 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 205248 82 None -1 27 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
2543 3681 68 None -1023 14 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
5358 3681 68 None -1023 14 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
54 3681 68 None -1023 14 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
CHEMBL128 3681 68 None -1023 14 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
DB00669 3681 68 None -1023 14 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
443955 204347 92 None -11 8 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 350 3 0 4 4.1 CCOC(=O)C1=C[C@]2(CC)CCCN3CCc4c(n1c1ccccc41)[C@@H]32 10.1038/s41467-023-40064-9
CHEMBL71752 204347 92 None -11 8 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 350 3 0 4 4.1 CCOC(=O)C1=C[C@]2(CC)CCCN3CCc4c(n1c1ccccc41)[C@@H]32 10.1038/s41467-023-40064-9
5357 98708 41 None -117 5 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 7 1 5 1.7 CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)ccc1OC 10.1038/s41467-023-40064-9
CHEMBL277945 98708 41 None -117 5 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 7 1 5 1.7 CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)ccc1OC 10.1038/s41467-023-40064-9
16351 102703 47 None -208 17 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102703 47 None -208 17 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
57469 18834 125 None -10 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1282 18834 125 None -10 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 10.1038/s41467-023-40064-9
2286 3161 51 None -40 28 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3161 51 None -40 28 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3161 51 None -40 28 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3161 51 None -40 28 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3161 51 None -40 28 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
2393 3309 82 None -2511 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
5078 3309 82 None -2511 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
51 3309 82 None -2511 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
CHEMBL905 3309 82 None -2511 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
DB00953 3309 82 None -2511 9 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
4046 2466 33 None -33 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2466 33 None -33 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2466 33 None -33 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2466 33 None -33 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
104850 3305 96 None -1230 28 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3305 96 None -1230 28 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3305 96 None -1230 28 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3305 96 None -1230 28 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3305 96 None -1230 28 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
1056 3346 116 None -25 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
2405 3346 116 None -25 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
77999 3346 116 None -25 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
CHEMBL121 3346 116 None -25 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
DB00412 3346 116 None -25 10 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
24776445 3966 115 None -1778 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 4 1 4 4.7 O=C(c1ccc(cc1Cl)S(=O)(=O)C)Nc1ccc(c(c1)c1ccccn1)Cl 10.1038/s41467-023-40064-9
4227 3966 115 None -1778 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 4 1 4 4.7 O=C(c1ccc(cc1Cl)S(=O)(=O)C)Nc1ccc(c(c1)c1ccccn1)Cl 10.1038/s41467-023-40064-9
6975 3966 115 None -1778 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 4 1 4 4.7 O=C(c1ccc(cc1Cl)S(=O)(=O)C)Nc1ccc(c(c1)c1ccccn1)Cl 10.1038/s41467-023-40064-9
CHEMBL473417 3966 115 None -1778 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 4 1 4 4.7 O=C(c1ccc(cc1Cl)S(=O)(=O)C)Nc1ccc(c(c1)c1ccccn1)Cl 10.1038/s41467-023-40064-9
DB08828 3966 115 None -1778 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 4 1 4 4.7 O=C(c1ccc(cc1Cl)S(=O)(=O)C)Nc1ccc(c(c1)c1ccccn1)Cl 10.1038/s41467-023-40064-9
3081361 93905 123 None -22 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93905 123 None -22 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
2372 106441 40 None -537 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL314010 106441 40 None -537 6 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
71731823 111678 61 None -11 3 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 0 1 7 2.8 C[C@H]1Oc2cc(cnc2N)-c2c(nn(C)c2C#N)CN(C)C(=O)c2ccc(F)cc21 10.1038/s41467-023-40064-9
CHEMBL3286830 111678 61 None -11 3 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 0 1 7 2.8 C[C@H]1Oc2cc(cnc2N)-c2c(nn(C)c2C#N)CN(C)C(=O)c2ccc(F)cc21 10.1038/s41467-023-40064-9
3074 17926 26 None -12 7 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL126075 17926 26 None -12 7 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL508338 188942 0 None -218 15 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL None None None None 10.1038/s41467-023-40064-9
2105 3032 37 None -3 25 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 3032 37 None -3 25 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 3032 37 None -3 25 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 3032 37 None -3 25 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 3032 37 None -3 25 Human 7.8 pAC50 = 7.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
11658860 2329 51 None -35 11 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
2941 2329 51 None -35 11 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
4374 2329 51 None -35 11 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
CHEMBL360328 2329 51 None -35 11 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
DB04871 2329 51 None -35 11 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
124087 1377 114 None -1 27 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1377 114 None -1 27 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1377 114 None -1 27 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1377 114 None -1 27 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1377 114 None -1 27 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
2165 203760 71 None 3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
3647519 203760 71 None 3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
CHEMBL682 203760 71 None 3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
3108 207264 116 None -7 7 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 504 12 4 12 -0.0 OCCN(CCO)c1nc(N2CCCCC2)c2nc(N(CCO)CCO)nc(N3CCCCC3)c2n1 10.1038/s41467-023-40064-9
CHEMBL932 207264 116 None -7 7 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 504 12 4 12 -0.0 OCCN(CCO)c1nc(N2CCCCC2)c2nc(N(CCO)CCO)nc(N3CCCCC3)c2n1 10.1038/s41467-023-40064-9
1209 1645 75 None -56 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1645 75 None -56 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1645 75 None -56 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1645 75 None -56 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1645 75 None -56 20 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
260 3840 54 None -15 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2775 3840 54 None -15 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
656665 3840 54 None -15 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL56564 3840 54 None -15 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB11699 3840 54 None -15 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
4497 34374 99 None -9 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 8 1 8 3.0 COCCOC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL1428 34374 99 None -9 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 8 1 8 3.0 COCCOC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
3823 50191 42 None -38 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
76973198 50191 42 None -38 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL157101 50191 42 None -38 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
10831 116937 25 None -3 6 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL338667 116937 25 None -3 6 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
3488 179112 115 None -120 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 493 8 3 5 3.6 COc1ccc(Cl)cc1C(=O)NCCc1ccc(S(=O)(=O)NC(=O)NC2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL472 179112 115 None -120 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 493 8 3 5 3.6 COc1ccc(Cl)cc1C(=O)NCCc1ccc(S(=O)(=O)NC(=O)NC2CCCCC2)cc1 10.1038/s41467-023-40064-9
636403 188244 22 None -6 7 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL499915 188244 22 None -6 7 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
31703 194694 63 None -23 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL359744 194694 63 None -23 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL53463 194694 63 None -23 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
2333 142310 97 None -1 14 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
CHEMBL388590 142310 97 None -1 14 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
2169 44817 35 None -26 12 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
CHEMBL152231 44817 35 None -26 12 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
5453 203596 102 None -36 14 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
CHEMBL671 203596 102 None -36 14 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
19861 207500 50 None -75 10 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
CHEMBL946 207500 50 None -75 10 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
137 369 52 None -7244 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
2119 369 52 None -7244 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
563 369 52 None -7244 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
66368 369 52 None -7244 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
CHEMBL266195 369 52 None -7244 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
DB00866 369 52 None -7244 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
2541 783 120 None -8511 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O 10.1038/s41467-023-40064-9
587 783 120 None -8511 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O 10.1038/s41467-023-40064-9
6907 783 120 None -8511 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1016 783 120 None -8511 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O 10.1038/s41467-023-40064-9
DB00796 783 120 None -8511 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O 10.1038/s41467-023-40064-9
DB13919 783 120 None -8511 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O 10.1038/s41467-023-40064-9
4942 5686 50 None -19 11 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1078261 5686 50 None -19 11 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
10102 2529 88 None -1548 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
1824 2529 88 None -1548 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
65906 2529 88 None -1548 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
CHEMBL94454 2529 88 None -1548 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
DB12523 2529 88 None -1548 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
41684 31191 105 None -38 32 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31191 105 None -38 32 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
4499 59745 99 None -8 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
CHEMBL1726 59745 99 None -8 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
37367 8619 14 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 2 0 4 3.2 CN(C)C(=O)OC1N=C(c2ccccc2)c2cc(Cl)ccc2N(C)C1=O 10.1038/s41467-023-40064-9
CHEMBL1095282 8619 14 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 2 0 4 3.2 CN(C)C(=O)OC1N=C(c2ccccc2)c2cc(Cl)ccc2N(C)C1=O 10.1038/s41467-023-40064-9
11954369 189059 24 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 394 2 2 4 2.7 C[C@@H]1C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@H]1C(=O)CO 10.1038/s41467-023-40064-9
CHEMBL509924 189059 24 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 394 2 2 4 2.7 C[C@@H]1C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@H]1C(=O)CO 10.1038/s41467-023-40064-9
5991 203896 72 None -3 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL691 203896 72 None -3 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
4760 204226 84 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 222 1 0 2 2.8 O=C1c2ccccc2C(=O)C1c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL711 204226 84 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 222 1 0 2 2.8 O=C1c2ccccc2C(=O)C1c1ccccc1 10.1038/s41467-023-40064-9
4452 2742 19 None -107 21 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2742 19 None -107 21 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2742 19 None -107 21 Human 6.8 pAC50 = 6.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
3294 1993 111 None -1862 23 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 1993 111 None -1862 23 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 1993 111 None -1862 23 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 1993 111 None -1862 23 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 1993 111 None -1862 23 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
214 3831 58 None -26 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3831 58 None -26 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3831 58 None -26 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3831 58 None -26 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3831 58 None -26 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3831 58 None -26 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
37 775 60 None -3 12 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 775 60 None -3 12 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 775 60 None -3 12 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 775 60 None -3 12 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 775 60 None -3 12 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
57469 18834 125 None -10 6 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1282 18834 125 None -10 6 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 10.1038/s41467-023-40064-9
46220502 112556 84 None -61 4 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 506 7 1 8 4.9 CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1 10.1038/s41467-023-40064-9
CHEMBL3301610 112556 84 None -61 4 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 506 7 1 8 4.9 CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1 10.1038/s41467-023-40064-9
44112 121264 48 None -478 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL357995 121264 48 None -478 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
2099 9275 55 None 52 5 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O 10.1038/s41467-023-40064-9
CHEMBL1110 9275 55 None 52 5 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O 10.1038/s41467-023-40064-9
68867 78144 38 None 1 13 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL2104523 78144 38 None 1 13 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
43815 186896 64 None -125 20 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 186896 64 None -125 20 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 186896 64 None -125 20 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
60606 61530 73 None 1 8 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 321 3 0 4 3.7 COC(=O)[C@H](c1ccccc1Cl)N1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1771 61530 73 None 1 8 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 321 3 0 4 3.7 COC(=O)[C@H](c1ccccc1Cl)N1CCc2sccc2C1 10.1038/s41467-023-40064-9
5591 157507 90 None 1 17 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
CHEMBL408 157507 90 None 1 17 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
4046 2466 33 None -33 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2466 33 None -33 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2466 33 None -33 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2466 33 None -33 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
108000 56823 39 None -58 5 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
135418340 56823 39 None -58 5 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1643895 56823 39 None -58 5 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 2 1 3 2.9 Cn1cc(C(=O)[C@@H]2CCc3[nH]cnc3C2)c2ccccc21 10.1038/s41467-023-40064-9
445643 97360 69 None -2 7 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
CHEMBL269732 97360 69 None -2 7 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
5639 98867 75 None -398 13 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
CHEMBL279229 98867 75 None -398 13 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
198 312 126 None -724 4 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
82148 312 126 None -724 4 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
99 312 126 None -724 4 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
CHEMBL10878 312 126 None -724 4 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
DB06594 312 126 None -724 4 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
2726 916 68 None -134 42 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 916 68 None -134 42 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 916 68 None -134 42 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 916 68 None -134 42 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 916 68 None -134 42 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2473 163159 47 None -2454 4 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 5 2 4 1.7 CC(C)(C)NCC(O)COc1ccccc1C#N 10.1038/s41467-023-40064-9
CHEMBL418134 163159 47 None -2454 4 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 5 2 4 1.7 CC(C)(C)NCC(O)COc1ccccc1C#N 10.1038/s41467-023-40064-9
168871 89101 14 None -630 13 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL2365712 89101 14 None -630 13 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
3752 27000 82 None - 1 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 1 2 5 2.0 Nc1nc(N)nc(-c2cc(Cl)ccc2Cl)n1 10.1038/s41467-023-40064-9
CHEMBL136497 27000 82 None - 1 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 1 2 5 2.0 Nc1nc(N)nc(-c2cc(Cl)ccc2Cl)n1 10.1038/s41467-023-40064-9
6010 30667 44 None 1 2 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 302 0 1 2 4.3 C[C@]12CCC(=O)C=C1CC[C@@H]1[C@@H]2CC[C@@]2(C)[C@H]1CC[C@]2(C)O 10.1038/s41467-023-40064-9
CHEMBL1395 30667 44 None 1 2 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 302 0 1 2 4.3 C[C@]12CCC(=O)C=C1CC[C@@H]1[C@@H]2CC[C@@]2(C)[C@H]1CC[C@]2(C)O 10.1038/s41467-023-40064-9
146570 43424 67 None -6 7 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1508 43424 67 None -6 7 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
1400 1944 70 None -4 16 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1944 70 None -4 16 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1944 70 None -4 16 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1944 70 None -4 16 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1944 70 None -4 16 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1944 70 None -4 16 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
4150 785 39 None -35 15 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5288 785 39 None -35 15 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019 785 39 None -35 15 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
CHEMBL190461 785 39 None -35 15 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
DB09061 785 39 None -35 15 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
2865 4112 73 None -23 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4112 73 None -23 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4112 73 None -23 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4112 73 None -23 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4112 73 None -23 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
4940 14438 35 None -7 15 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1201210 14438 35 None -7 15 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
2202 3110 96 None -38 10 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 3110 96 None -38 10 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 3110 96 None -38 10 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 3110 96 None -38 10 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 3110 96 None -38 10 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
3689 102744 55 None -331 16 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1372983 102744 55 None -331 16 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL305187 102744 55 None -331 16 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
4762 14437 27 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 177 1 1 2 1.7 CC1NCCOC1c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201208 14437 27 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 177 1 1 2 1.7 CC1NCCOC1c1ccccc1 10.1038/s41467-023-40064-9
445643 97360 69 None -2 7 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
CHEMBL269732 97360 69 None -2 7 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 803 7 3 12 4.6 C=CC[C@@H]1/C=C(\C)C[C@H](C)C[C@H](OC)[C@H]2O[C@@](O)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@H](/C(C)=C/[C@@H]3CC[C@@H](O)[C@H](OC)C3)[C@H](C)[C@@H](O)CC1=O)[C@H](C)C[C@@H]2OC 10.1038/s41467-023-40064-9
53232 188601 95 None -3548 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 1 5 4.2 CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL503 188601 95 None -3548 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 1 5 4.2 CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
448537 160226 89 None -28 31 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 160226 89 None -28 31 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
4756 16617 50 None -12 16 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1201022 16617 50 None -12 16 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1242 16617 50 None -12 16 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
27812 66961 43 None -2 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 308 1 1 2 3.7 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3C=C[C@@]21CC 10.1038/s41467-023-40064-9
CHEMBL1868702 66961 43 None -2 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 308 1 1 2 3.7 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3C=C[C@@]21CC 10.1038/s41467-023-40064-9
1153 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
12668023 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026874 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
30026875 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
3341 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
6603851 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
933 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
939 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
985 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1160786 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL1161520 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
CHEMBL588 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
DB00800 1615 58 None -28 12 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1038/s41467-023-40064-9
150 2492 21 None -2 17 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1764 2492 21 None -2 17 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226 2492 21 None -2 17 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
CHEMBL1201356 2492 21 None -2 17 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
DB00353 2492 21 None -2 17 Human 7.6 pAC50 = 7.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
31101 726 40 None -165 29 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 726 40 None -165 29 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 726 40 None -165 29 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 726 40 None -165 29 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 726 40 None -165 29 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
4046 2466 33 None -33 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2466 33 None -33 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2466 33 None -33 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2466 33 None -33 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
10007 14452 38 None 1 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 2 1 1 2.6 CC(C)(N)Cc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1201269 14452 38 None 1 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 183 2 1 1 2.6 CC(C)(N)Cc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
54841 203104 52 None -14 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL641 203104 52 None -14 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 10.1038/s41467-023-40064-9
1201549 594 24 None -208 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 594 24 None -208 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 594 24 None -208 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 594 24 None -208 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 594 24 None -208 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 594 24 None -208 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
68873 43534 64 None -2 3 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 366 0 0 3 4.3 C[C@]12CCC(=O)C=C1[C@@H]1C[C@@H]1[C@H]1[C@@H]3[C@@H]4C[C@@H]4[C@@]4(CCC(=O)O4)[C@@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL1509 43534 64 None -2 3 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 366 0 0 3 4.3 C[C@]12CCC(=O)C=C1[C@@H]1C[C@@H]1[C@H]1[C@@H]3[C@@H]4C[C@@H]4[C@@]4(CCC(=O)O4)[C@@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
319 1312 44 None -8317 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 1312 44 None -8317 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 1312 44 None -8317 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 1312 44 None -8317 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 1312 44 None -8317 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 1312 44 None -8317 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
4209 3141 75 None -22387 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 3141 75 None -22387 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 3141 75 None -22387 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 3141 75 None -22387 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 3141 75 None -22387 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 3141 75 None -22387 17 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL508338 188942 0 None -218 15 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None None 10.1038/s41467-023-40064-9
8730 195868 72 None -5 5 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 777 5 3 4 4.6 N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
90657408 195868 72 None -5 5 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 777 5 3 4 4.6 N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL559 195868 72 None -5 5 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 777 5 3 4 4.6 N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
4612 205957 39 None -3 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 5 3 5 1.8 CC(C)NCC1CCc2cc(CO)c([N+](=O)[O-])cc2N1 10.1038/s41467-023-40064-9
CHEMBL847 205957 39 None -3 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 279 5 3 5 1.8 CC(C)NCC1CCc2cc(CO)c([N+](=O)[O-])cc2N1 10.1038/s41467-023-40064-9
102 4096 48 None -16 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4096 48 None -16 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4096 48 None -16 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4096 48 None -16 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4096 48 None -16 20 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
26987 946 33 None -263 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 946 33 None -263 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 946 33 None -263 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 946 33 None -263 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 946 33 None -263 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
21722 17960 31 None -2 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17960 31 None -2 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
4450 178204 69 None -4 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL465026 178204 69 None -4 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
100 3776 58 None -125 38 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3776 58 None -125 38 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3776 58 None -125 38 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3776 58 None -125 38 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3776 58 None -125 38 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
124 2960 47 None -457 25 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
2032 2960 47 None -457 25 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
4636 2960 47 None -457 25 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL762 2960 47 None -457 25 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
DB00935 2960 47 None -457 25 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
2995 204382 53 None -154 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 204382 53 None -154 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 204382 53 None -154 18 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
2220 3112 82 None -10 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 3112 82 None -10 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 3112 82 None -10 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 3112 82 None -10 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 3112 82 None -10 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
11626560 200914 94 None 1 14 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 200914 94 None 1 14 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
213 3824 55 None -16 22 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 3824 55 None -16 22 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 3824 55 None -16 22 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 3824 55 None -16 22 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 3824 55 None -16 22 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2402 3345 62 None -512 17 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095 3345 62 None -512 17 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
7295 3345 62 None -512 17 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
CHEMBL589 3345 62 None -512 17 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
DB00268 3345 62 None -512 17 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
10531 1408 21 None -100 26 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 1408 21 None -100 26 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 1408 21 None -100 26 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 1408 21 None -100 26 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 1408 21 None -100 26 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
2274 3151 58 None -35 37 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3151 58 None -35 37 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3151 58 None -35 37 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3151 58 None -35 37 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3151 58 None -35 37 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3926 207218 40 None -4 18 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 207218 40 None -4 18 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
25271887 5128 84 None -7 2 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 159 5 2 2 1.1 CC(C)C[C@H](CN)CC(=O)O 10.1038/s41467-023-40064-9
5486971 5128 84 None -7 2 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 159 5 2 2 1.1 CC(C)C[C@H](CN)CC(=O)O 10.1038/s41467-023-40064-9
CHEMBL1059 5128 84 None -7 2 Human 4.6 pAC50 = 4.6 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 159 5 2 2 1.1 CC(C)C[C@H](CN)CC(=O)O 10.1038/s41467-023-40064-9
2351 4269 49 None -12 22 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4269 49 None -12 22 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4269 49 None -12 22 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
50922675 112557 54 None -3 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 539 9 3 9 3.9 COC(=O)N[C@@H](C)CNc1nccc(-c2cn(C(C)C)nc2-c2cc(Cl)cc(NS(C)(=O)=O)c2F)n1 10.1038/s41467-023-40064-9
CHEMBL3301612 112557 54 None -3 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 539 9 3 9 3.9 COC(=O)N[C@@H](C)CNc1nccc(-c2cn(C(C)C)nc2-c2cc(Cl)cc(NS(C)(=O)=O)c2F)n1 10.1038/s41467-023-40064-9
154257 178595 67 None -6 19 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178595 67 None -6 19 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
6127 14467 8 None -177 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1201340 14467 8 None -177 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
5833 30453 74 None -2 4 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 416 1 0 5 4.9 CC(=O)S[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@]34CCC(=O)O4)[C@H]12 10.1038/s41467-023-40064-9
CHEMBL1393 30453 74 None -2 4 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 416 1 0 5 4.9 CC(=O)S[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@]34CCC(=O)O4)[C@H]12 10.1038/s41467-023-40064-9
4413 98045 57 None -9 15 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 98045 57 None -9 15 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
5467 205905 43 None -46 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC 10.1038/s41467-023-40064-9
CHEMBL84158 205905 43 None -46 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC 10.1038/s41467-023-40064-9
5732 206912 59 None -138 4 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 3 0 3 3.2 Cc1ccc(-c2nc3ccc(C)cn3c2CC(=O)N(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL911 206912 59 None -138 4 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 3 0 3 3.2 Cc1ccc(-c2nc3ccc(C)cn3c2CC(=O)N(C)C)cc1 10.1038/s41467-023-40064-9
37 775 60 None -3 12 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 775 60 None -3 12 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 775 60 None -3 12 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 775 60 None -3 12 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 775 60 None -3 12 Human 8.5 pAC50 = 8.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HTR2B in an in vitro cell-based assay (CRO assay) measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
135 2515 43 None -5 33 Human 7.5 pAC50 = 7.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2515 43 None -5 33 Human 7.5 pAC50 = 7.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2515 43 None -5 33 Human 7.5 pAC50 = 7.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2515 43 None -5 33 Human 7.5 pAC50 = 7.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2515 43 None -5 33 Human 7.5 pAC50 = 7.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
168871 89101 14 None -630 13 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL2365712 89101 14 None -630 13 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
242 469 124 None -33 33 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 469 124 None -33 33 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 469 124 None -33 33 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 469 124 None -33 33 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 469 124 None -33 33 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
54477 84624 36 None -33 8 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
CHEMBL22242 84624 36 None -33 8 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
72093 35031 9 None -2 28 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35031 9 None -2 28 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35031 9 None -2 28 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
4066 204603 78 None -194 16 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 204603 78 None -194 16 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
2342 596 39 None 3 8 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
331 596 39 None 3 8 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
7124 596 39 None 3 8 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
CHEMBL1201250 596 39 None 3 8 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
DB00767 596 39 None 3 8 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC 10.1038/s41467-023-40064-9
24826799 10766 104 None -10 20 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10766 104 None -10 20 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
5411 204010 89 None -11220 11 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL698 204010 89 None -11220 11 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
135409453 3744 41 None -28 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3744 41 None -28 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3744 41 None -28 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
1481 2053 116 None -38904 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1038/s41467-023-40064-9
3749 2053 116 None -38904 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1038/s41467-023-40064-9
589 2053 116 None -38904 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1038/s41467-023-40064-9
6908 2053 116 None -38904 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1038/s41467-023-40064-9
CHEMBL1513 2053 116 None -38904 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1038/s41467-023-40064-9
DB01029 2053 116 None -38904 6 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1038/s41467-023-40064-9
1343 1876 62 None -79 12 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 1876 62 None -79 12 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 1876 62 None -79 12 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 1876 62 None -79 12 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 1876 62 None -79 12 Human 6.5 pAC50 = 6.5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
1440 2014 119 None -93 7 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1909 2014 119 None -93 7 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
3715 2014 119 None -93 7 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL6 2014 119 None -93 7 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB00328 2014 119 None -93 7 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
60198 14380 83 None -15 3 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 0 0 2 4.0 C=C1C[C@@H]2[C@H](CC[C@]3(C)C(=O)CC[C@@H]23)[C@@]2(C)C=CC(=O)C=C12 10.1038/s41467-023-40064-9
CHEMBL1200374 14380 83 None -15 3 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 0 0 2 4.0 C=C1C[C@@H]2[C@H](CC[C@]3(C)C(=O)CC[C@@H]23)[C@@]2(C)C=CC(=O)C=C12 10.1038/s41467-023-40064-9
5284550 41691 15 None -190 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41691 15 None -190 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
240 941 43 None -79 23 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
2769 941 43 None -79 23 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
44279790 941 43 None -79 23 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
660 941 43 None -79 23 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL1729 941 43 None -79 23 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL560739 941 43 None -79 23 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
DB00604 941 43 None -79 23 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
55645 84341 8 None -389 11 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
CHEMBL2218861 84341 8 None -389 11 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
4993 122331 110 None -5 5 Human 4.4 pAC50 = 4.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 248 2 2 4 2.5 CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL36 122331 110 None -5 5 Human 4.4 pAC50 = 4.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 248 2 2 4 2.5 CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
54454 5226 88 None -1 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL1064 5226 88 None -1 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
4976 203556 29 None -426 15 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL668 203556 29 None -426 15 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
134 2497 24 None 2 18 Human 8.4 pAC50 = 8.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 2497 24 None 2 18 Human 8.4 pAC50 = 8.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 2497 24 None 2 18 Human 8.4 pAC50 = 8.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 2497 24 None 2 18 Human 8.4 pAC50 = 8.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 2497 24 None 2 18 Human 8.4 pAC50 = 8.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
67462786 120491 56 None 2 6 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 446 9 1 8 4.2 COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1 10.1038/s41467-023-40064-9
CHEMBL3545376 120491 56 None 2 6 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 446 9 1 8 4.2 COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1 10.1038/s41467-023-40064-9
2337 3232 77 None -11 29 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3232 77 None -11 29 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3232 77 None -11 29 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3232 77 None -11 29 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3232 77 None -11 29 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
2407 3347 76 None -128 17 Human 6.4 pAC50 = 6.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3347 76 None -128 17 Human 6.4 pAC50 = 6.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3347 76 None -128 17 Human 6.4 pAC50 = 6.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3347 76 None -128 17 Human 6.4 pAC50 = 6.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3347 76 None -128 17 Human 6.4 pAC50 = 6.4 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
1782 2501 84 None -45 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
241 2501 84 None -45 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
4168 2501 84 None -45 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
CHEMBL86 2501 84 None -45 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
DB01233 2501 84 None -45 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
2600 3750 74 None -15 32 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3750 74 None -15 32 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3750 74 None -15 32 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3750 74 None -15 32 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3750 74 None -15 32 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
392622 56282 95 None -3 20 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56282 95 None -3 20 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
25382 9125 37 None -117 21 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9125 37 None -117 21 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
441243 9804 58 None -288 11 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
CHEMBL114 9804 58 None -288 11 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
3463 175122 107 None 3 4 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 250 6 1 2 3.6 Cc1ccc(C)c(OCCCC(C)(C)C(=O)O)c1 10.1038/s41467-023-40064-9
CHEMBL457 175122 107 None 3 4 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 250 6 1 2 3.6 Cc1ccc(C)c(OCCCC(C)(C)C(=O)O)c1 10.1038/s41467-023-40064-9
2389 3306 118 None -91 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3306 118 None -91 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3306 118 None -91 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3306 118 None -91 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3306 118 None -91 29 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
17676 7040 29 None -1023 13 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5281082 7040 29 None -1023 13 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1085 7040 29 None -1023 13 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
16362 3103 71 None -371 35 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3103 71 None -371 35 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3103 71 None -371 35 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3103 71 None -371 35 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3103 71 None -371 35 Human 4.4 pAC50 = 4.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
11561674 189587 83 None - 1 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 460 8 1 7 2.4 CCOc1cc([C@@H](CS(C)(=O)=O)N2C(=O)c3cccc(NC(C)=O)c3C2=O)ccc1OC 10.1038/s41467-023-40064-9
CHEMBL514800 189587 83 None - 1 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 460 8 1 7 2.4 CCOc1cc([C@@H](CS(C)(=O)=O)N2C(=O)c3cccc(NC(C)=O)c3C2=O)ccc1OC 10.1038/s41467-023-40064-9
135398737 955 93 None -8 43 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 955 93 None -8 43 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 955 93 None -8 43 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 955 93 None -8 43 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 955 93 None -8 43 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
1222 1651 49 None -107 25 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1651 49 None -107 25 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1651 49 None -107 25 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1651 49 None -107 25 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1651 49 None -107 25 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
228 444 28 None -575 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 444 28 None -575 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 444 28 None -575 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 444 28 None -575 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 444 28 None -575 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
19675 51640 43 None -363 15 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1584 51640 43 None -363 15 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
49806720 60050 99 None 1 4 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 482 3 1 5 4.8 CCc1cc2c(cc1N1CCC(N3CCOCC3)CC1)C(C)(C)c1[nH]c3cc(C#N)ccc3c1C2=O 10.1038/s41467-023-40064-9
CHEMBL1738797 60050 99 None 1 4 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 482 3 1 5 4.8 CCc1cc2c(cc1N1CCC(N3CCOCC3)CC1)C(C)(C)c1[nH]c3cc(C#N)ccc3c1C2=O 10.1038/s41467-023-40064-9
212 3777 47 None -758 22 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3777 47 None -758 22 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3777 47 None -758 22 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3777 47 None -758 22 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3777 47 None -758 22 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2318 154832 29 None 3 15 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154832 29 None 3 15 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
1427 2000 54 None -1621 30 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2000 54 None -1621 30 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2000 54 None -1621 30 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2000 54 None -1621 30 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2000 54 None -1621 30 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
165193 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
2303 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4946 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
564 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
62882 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
63 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
66366 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
91536 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL27 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL452861 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
DB00571 3165 68 None -407 20 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
5329102 194703 86 None -8 37 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194703 86 None -8 37 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
2470 3626 50 None -30902 23 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3626 50 None -30902 23 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3626 50 None -30902 23 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3626 50 None -30902 23 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3626 50 None -30902 23 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3704 78160 41 None 3 5 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 231 3 1 3 1.6 C1=Cc2cccc(OCC3CNCCO3)c2C1 10.1038/s41467-023-40064-9
CHEMBL2105022 78160 41 None 3 5 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 231 3 1 3 1.6 C1=Cc2cccc(OCC3CNCCO3)c2C1 10.1038/s41467-023-40064-9
2585 800 103 None -64 34 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 800 103 None -64 34 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 800 103 None -64 34 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 800 103 None -64 34 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 800 103 None -64 34 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
31101 726 40 None -165 29 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 726 40 None -165 29 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 726 40 None -165 29 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 726 40 None -165 29 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 726 40 None -165 29 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
135398745 2893 112 None -4 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2893 112 None -4 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2893 112 None -4 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2893 112 None -4 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
2267 557 71 None -223 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 557 71 None -223 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 557 71 None -223 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 557 71 None -223 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 557 71 None -223 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3042 1402 35 None -1096 17 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1402 35 None -1096 17 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1402 35 None -1096 17 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1402 35 None -1096 17 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1402 35 None -1096 17 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
4199 98817 42 None -9 3 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 5 1 5 2.2 Cc1cc(-c2ccccc2)nnc1NCCN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL278819 98817 42 None -9 3 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 5 1 5 2.2 Cc1cc(-c2ccccc2)nnc1NCCN1CCOCC1 10.1038/s41467-023-40064-9
2398 951 62 None -831 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 951 62 None -831 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 951 62 None -831 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 951 62 None -831 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 951 62 None -831 36 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2284 3160 33 None -89 34 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3160 33 None -89 34 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3160 33 None -89 34 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3160 33 None -89 34 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3160 33 None -89 34 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
5803 162203 84 None -1 8 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 622 4 2 3 4.6 O=C(O)Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1 10.1038/s41467-023-40064-9
CHEMBL41632 162203 84 None -1 8 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 622 4 2 3 4.6 O=C(O)Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1 10.1038/s41467-023-40064-9
1170 1620 75 None -109 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
3348 1620 75 None -109 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
4819 1620 75 None -109 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
74685737 1620 75 None -109 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
CHEMBL914 1620 75 None -109 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
DB00950 1620 75 None -109 5 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
2601 3751 33 None -186 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
443951 3751 33 None -186 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
56 3751 33 None -186 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL73151 3751 33 None -186 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB13399 3751 33 None -186 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
25102847 78192 93 None -4 10 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2105717 78192 93 None -4 10 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
3949 100586 50 None -6 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100586 50 None -6 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
2435 3563 83 None -20 21 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3563 83 None -20 21 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3563 83 None -20 21 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3563 83 None -20 21 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3563 83 None -20 21 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
2136 3073 30 None -120 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 3073 30 None -120 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 3073 30 None -120 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 3073 30 None -120 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 3073 30 None -120 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
2367 961 86 None -6 6 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 10.1038/s41467-023-40064-9
6167 961 86 None -6 6 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 10.1038/s41467-023-40064-9
726 961 86 None -6 6 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 10.1038/s41467-023-40064-9
CHEMBL107 961 86 None -6 6 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 10.1038/s41467-023-40064-9
DB01394 961 86 None -6 6 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 399 5 1 6 2.9 COc1c(OC)cc2c(c1OC)c1ccc(c(=O)cc1[C@H](CC2)NC(=O)C)OC 10.1038/s41467-023-40064-9
2247 504 81 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 504 81 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 504 81 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 504 81 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 504 81 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
3157 1458 71 None -1318 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 1458 71 None -1318 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 1458 71 None -1318 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 1458 71 None -1318 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 1458 71 None -1318 22 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL4743867 214010 14 None -20 15 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
3062316 33545 121 None -1 10 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL1421 33545 121 None -1 10 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
2583 3747 118 None -3548 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
592 3747 118 None -3548 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999 3747 118 None -3548 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
CHEMBL1017 3747 118 None -3548 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
DB00966 3747 118 None -3548 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
103 4122 61 None -6 22 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4122 61 None -6 22 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4122 61 None -6 22 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4122 61 None -6 22 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4122 61 None -6 22 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
129211 3722 78 None -14125 14 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
2562 3722 78 None -14125 14 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
488 3722 78 None -14125 14 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
CHEMBL836 3722 78 None -14125 14 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
DB00706 3722 78 None -14125 14 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
16363 593 53 None -1258 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 593 53 None -1258 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 593 53 None -1258 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 593 53 None -1258 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 593 53 None -1258 21 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
92727 204529 77 None -1 6 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 628 15 4 5 4.3 Cc1cccc(C)c1OCC(=O)N[C@@H](Cc1ccccc1)[C@@H](O)C[C@H](Cc1ccccc1)NC(=O)[C@H](C(C)C)N1CCCNC1=O 10.1038/s41467-023-40064-9
CHEMBL729 204529 77 None -1 6 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 628 15 4 5 4.3 Cc1cccc(C)c1OCC(=O)N[C@@H](Cc1ccccc1)[C@@H](O)C[C@H](Cc1ccccc1)NC(=O)[C@H](C(C)C)N1CCCNC1=O 10.1038/s41467-023-40064-9
11504295 2902 47 None -50118 8 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
4814 2902 47 None -50118 8 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
7543 2902 47 None -50118 8 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
CHEMBL605846 2902 47 None -50118 8 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
DB09080 2902 47 None -50118 8 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
2782 31970 67 None -199 8 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
CHEMBL1407943 31970 67 None -199 8 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
CHEMBL3216363 31970 67 None -199 8 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
1353 1898 93 None -831 39 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1898 93 None -831 39 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1898 93 None -831 39 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1898 93 None -831 39 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1898 93 None -831 39 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
2771 194994 74 None -5 16 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 194994 74 None -5 16 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 194994 74 None -5 16 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
1816 2523 102 None -1047 12 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205 2523 102 None -1047 12 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
7241 2523 102 None -1047 12 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
CHEMBL654 2523 102 None -1047 12 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
DB00370 2523 102 None -1047 12 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4485 69350 118 None -42 11 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
CHEMBL193 69350 118 None -42 11 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
4567 9916 34 None -41 12 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL114655 9916 34 None -41 12 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
179 399 115 None -102 8 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
2159 399 115 None -102 8 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
963 399 115 None -102 8 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
CHEMBL243712 399 115 None -102 8 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
DB06288 399 115 None -102 8 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
213046 2370 59 None -4 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 2370 59 None -4 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 2370 59 None -4 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 2370 59 None -4 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 2370 59 None -4 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
1971 2846 38 None -165 32 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2846 38 None -165 32 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2846 38 None -165 32 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2846 38 None -165 32 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2846 38 None -165 32 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2448 99295 70 None -331 15 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 99295 70 None -331 15 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
1830 2572 44 None -8 11 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 2572 44 None -8 11 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 2572 44 None -8 11 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 2572 44 None -8 11 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 2572 44 None -8 11 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
2477 742 59 None -104 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
36 742 59 None -104 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
437 742 59 None -104 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
CHEMBL49 742 59 None -104 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
DB00490 742 59 None -104 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
5906 14463 23 None 1 4 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 2 3 3 0.8 C[C@H](N)[C@H](O)c1cccc(O)c1 10.1038/s41467-023-40064-9
CHEMBL1201319 14463 23 None 1 4 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 167 2 3 3 0.8 C[C@H](N)[C@H](O)c1cccc(O)c1 10.1038/s41467-023-40064-9
54682461 84657 62 None -1 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL222559 84657 62 None -1 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
68617 205504 62 None -14 30 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 205504 62 None -14 30 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 205504 62 None -14 30 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
20628 96519 28 None 1 13 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
CHEMBL26291 96519 28 None 1 13 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
209 3035 97 None -338 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2113 3035 97 None -338 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4748 3035 97 None -338 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL567 3035 97 None -338 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00850 3035 97 None -338 14 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2540 4369 111 None -1122 28 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 4369 111 None -1122 28 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
1212 1649 50 None -60 35 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 1649 50 None -60 35 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 1649 50 None -60 35 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 1649 50 None -60 35 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 1649 50 None -60 35 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
71496458 115538 87 None -2 16 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115538 87 None -2 16 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
4418 34192 85 None -3 18 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 34192 85 None -3 18 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
2880 97980 49 None -8 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL27289 97980 49 None -8 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
4178 195780 63 None 3 2 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N 10.1038/s41467-023-40064-9
CHEMBL558 195780 63 None 3 2 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N 10.1038/s41467-023-40064-9
1234 189197 56 None 9 10 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1256940 189197 56 None 9 10 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL51149 189197 56 None 9 10 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
6018 11033 96 None 2 3 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 10.1038/s41467-023-40064-9
CHEMBL117785 11033 96 None 2 3 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 10.1038/s41467-023-40064-9
118422671 2737 65 None -2884 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2737 65 None -2884 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2737 65 None -2884 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2737 65 None -2884 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2737 65 None -2884 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2737 65 None -2884 23 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
11980903 14460 19 None -239 25 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14460 19 None -239 25 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14460 19 None -239 25 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14460 19 None -239 25 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
138106885 166887 75 None -4 8 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C 10.1038/s41467-023-40064-9
36314 166887 75 None -4 8 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C 10.1038/s41467-023-40064-9
CHEMBL428647 166887 75 None -4 8 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C 10.1038/s41467-023-40064-9
5282175 14400 36 None 6 4 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL1200661 14400 36 None 6 4 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 424 16 2 5 5.1 CCCCCCCC(=O)CC[C@@H]1[C@@H](C/C=C\CCCC(=O)OC(C)C)[C@@H](O)C[C@H]1O 10.1038/s41467-023-40064-9
1530 2169 50 None -3 25 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827 2169 50 None -3 25 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
7206 2169 50 None -3 25 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
CHEMBL534 2169 50 None -3 25 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
DB00920 2169 50 None -3 25 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
5311507 194792 41 None -10 12 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL53904 194792 41 None -10 12 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
216416 111554 48 None -19 23 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111554 48 None -19 23 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
65700 78231 28 None -2 8 Human 6.0 pAC50 = 6.0 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2106919 78231 28 None -2 8 Human 6.0 pAC50 = 6.0 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
2291 3162 58 None -17 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
2561 3162 58 None -17 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
4932 3162 58 None -17 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL631 3162 58 None -17 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
DB01182 3162 58 None -17 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
5472 205795 75 None -16 16 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 205795 75 None -16 16 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 205795 75 None -16 16 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
2780 110502 36 None -9 11 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL325109 110502 36 None -9 11 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2B in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
43815 186896 64 None -125 20 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 186896 64 None -125 20 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 186896 64 None -125 20 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human HTR2B in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
5 139 72 None -2 27 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
5202 139 72 None -2 27 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
CHEMBL39 139 72 None -2 27 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
DB08839 139 72 None -2 27 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2020.127511
5 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 72 None -2 27 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5 139 72 None -2 27 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
5202 139 72 None -2 27 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
CHEMBL39 139 72 None -2 27 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
DB08839 139 72 None -2 27 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
4376990 192985 5 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192985 5 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192985 5 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
4376990 192985 5 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192985 5 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192985 5 None -1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
5 139 72 None -2 27 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
5202 139 72 None -2 27 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
CHEMBL39 139 72 None -2 27 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
DB08839 139 72 None -2 27 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
5 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
5202 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
CHEMBL39 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
DB08839 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
439280 119993 107 None -25 9 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
6971044 119993 107 None -25 9 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
CHEMBL350221 119993 107 None -25 9 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
5 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 139 72 None -2 27 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
439280 119993 107 None -25 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
6971044 119993 107 None -25 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
CHEMBL350221 119993 107 None -25 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
168293874 192155 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192155 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168293874 192155 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192155 0 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
5 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
5202 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL39 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
DB08839 139 72 None -2 27 Human 8.8 pEC50 = 8.8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
166 3334 18 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
3045227 3334 18 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
CHEMBL76781 3334 18 None 2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm0709034
4407909 192842 1 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192842 1 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192842 1 None 1 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44315993 172853 0 None 2 3 Human 8.0 pEC50 = 8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL451543 172853 0 None 2 3 Human 8.0 pEC50 = 8 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
4407909 192842 1 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192842 1 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192842 1 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
16115269 138104 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL376676 138104 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
9881885 64079 0 None -19 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180815 64079 0 None -19 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
17954204 63908 23 None -81 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
CHEMBL180668 63908 23 None -81 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
10465263 64302 63 None -89 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL181172 64302 63 None -89 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
11938 2396 7 None -75 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2bAgonist activity at human 5HT2b
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 2396 7 None -75 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2bAgonist activity at human 5HT2b
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 2396 7 None -75 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2bAgonist activity at human 5HT2b
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
59312249 111645 0 None -8 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(C(C)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286565 111645 0 None -8 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 282 3 2 4 2.4 CNc1nc(C(C)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
122442324 138325 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138325 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138325 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11658860 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
2941 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
4374 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL360328 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
DB04871 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
10379910 63271 0 None -6 2 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.3 COc1cc2c(cc1Br)C(C(C)C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179329 63271 0 None -6 2 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.3 COc1cc2c(cc1Br)C(C(C)C)CNCC2 10.1016/j.bmcl.2004.12.080
17954204 63908 23 None -81 3 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180668 63908 23 None -81 3 Human 6.0 pEC50 = 6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2004.12.080
122442324 138325 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138325 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138325 0 None -12 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11493484 89041 0 None -23 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337106 89041 0 None -23 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365079 89041 0 None -23 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
46230097 199343 0 None -6 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590816 199343 0 None -6 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
122442251 138335 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 138335 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 138335 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
4312735 192850 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192850 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192850 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
4312735 192850 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192850 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192850 1 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
122442251 138335 0 None -15 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770225 138335 0 None -15 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771396 138335 0 None -15 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573155 189135 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 4 2 3 1.1 O=S(=O)(NCC1CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL511044 189135 0 None 6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 4 2 3 1.1 O=S(=O)(NCC1CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
168282202 192860 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192860 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192860 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168282202 192860 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192860 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192860 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
44412404 77739 6 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209106 77739 6 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 206 1 1 2 1.6 Fc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
70693928 74456 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
CHEMBL2022192 74456 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
CHEMBL2028036 74456 0 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 253 5 1 2 3.3 NC[C@H]1C[C@@H]1c1ccccc1OCc1ccccc1 10.1021/ml200206z
162652937 183638 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4751981 183638 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802812 183638 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
5 139 72 None -2 27 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
5202 139 72 None -2 27 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
CHEMBL39 139 72 None -2 27 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
DB08839 139 72 None -2 27 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2009.07.063
168 3951 15 None 3 5 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
6604042 3951 15 None 3 5 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
CHEMBL309760 3951 15 None 3 5 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
157 2056 7 None 2 3 Rat 7.9 pEC50 = 7.9 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
9840090 2056 7 None 2 3 Rat 7.9 pEC50 = 7.9 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
CHEMBL134519 2056 7 None 2 3 Rat 7.9 pEC50 = 7.9 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
157 2056 7 None 2 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
9840090 2056 7 None 2 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
CHEMBL134519 2056 7 None 2 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1016/j.bmcl.2007.03.073
10465263 64302 63 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL181172 64302 63 None -89 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
162652937 183638 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4751981 183638 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802812 183638 0 None -67 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
134265627 163989 0 None -602 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1cccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)c1 10.1021/acsmedchemlett.8b00328
CHEMBL4208452 163989 0 None -602 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1cccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)c1 10.1021/acsmedchemlett.8b00328
53324327 56820 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
CHEMBL1643857 56820 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)ccn1 10.1016/j.bmcl.2010.11.089
44572176 12528 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1 10.1021/jm801354e
CHEMBL1186735 12528 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1 10.1021/jm801354e
CHEMBL475641 12528 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 2 1 1 2.8 Cc1ccc([C@H]2C[C@@H]2CN)c(Br)c1 10.1021/jm801354e
44572207 12670 0 None -8 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL1187556 12670 0 None -8 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
CHEMBL508680 12670 0 None -8 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 2 1 1 2.9 Cc1ccc(Cl)c([C@H]2C[C@@H]2CN)c1F 10.1021/jm801354e
11492162 72024 3 None -11 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197646 72024 3 None -11 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
53317924 56821 0 None -6 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 406 4 1 7 1.7 CC(=O)N(C)c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643858 56821 0 None -6 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 406 4 1 7 1.7 CC(=O)N(C)c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
44572180 12530 1 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
CHEMBL1186737 12530 1 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
CHEMBL475643 12530 1 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1ccc([C@H]2C[C@@H]2CN)cc1C 10.1021/jm801354e
11151653 91072 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397896 91072 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
54587668 61429 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770378 61429 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
1355 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
142 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
CHEMBL478 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
DB12110 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.063
44573156 187273 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 254 2 1 3 0.6 CN(C)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492949 187273 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 254 2 1 3 0.6 CN(C)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
1355 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
142 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
CHEMBL478 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
DB12110 1998 88 None -5 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.07.136
168285159 192890 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 192890 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 192890 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
23652278 62601 17 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL178365 62601 17 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
11608308 64279 4 None -407 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL181076 64279 4 None -407 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
162658803 183668 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759878 183668 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803107 183668 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
168285159 192890 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 192890 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 192890 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162658803 183668 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759878 183668 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803107 183668 0 None -14 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
134265732 163783 0 None -1000 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4206126 163783 0 None -1000 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 285 2 1 3 2.3 FC(F)(F)CCc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
134265665 164775 0 None -1047 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4218374 164775 0 None -1047 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 231 2 1 3 1.8 CCCc1cncc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
44572751 12467 1 None -16 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL1186509 12467 1 None -16 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL467736 12467 1 None -16 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
53321948 56774 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643677 56774 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
189 3466 39 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jmedchem.0c00424
5163 3466 39 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jmedchem.0c00424
CHEMBL297784 3466 39 None -1 4 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jmedchem.0c00424
44431699 88260 0 None 5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 315 4 1 6 1.7 Cc1noc(Cc2c3c(c(C[C@@H](C)N)c4c2OCC4)OCC3)n1 10.1016/j.bmcl.2007.03.073
CHEMBL234837 88260 0 None 5 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 315 4 1 6 1.7 Cc1noc(Cc2c3c(c(C[C@@H](C)N)c4c2OCC4)OCC3)n1 10.1016/j.bmcl.2007.03.073
10015414 63455 0 None -32 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 259 1 1 2 3.0 COc1cc2c(cc1C(F)(F)F)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179915 63455 0 None -32 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 259 1 1 2 3.0 COc1cc2c(cc1C(F)(F)F)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
16115271 79079 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL2113264 79079 0 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
44572168 12452 1 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
CHEMBL1186458 12452 1 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
CHEMBL464475 12452 1 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/jm801354e
10036629 64607 0 None -9 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL181787 64607 0 None -9 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
23652278 62601 17 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178365 62601 17 None -83 3 Human 5.9 pEC50 = 5.9 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 C[C@@H]1CNCCc2ccc(Cl)cc21 10.1016/j.bmcl.2004.12.080
25084025 12669 1 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL1187522 12669 1 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
CHEMBL506727 12669 1 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1cccc(Br)c1 10.1021/jm801354e
45484687 198441 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 339 3 1 5 1.9 O=c1cc2c(nn1Cc1ccccc1OC(F)(F)F)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL577410 198441 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 339 3 1 5 1.9 O=c1cc2c(nn1Cc1ccccc1OC(F)(F)F)CCNCC2 10.1016/j.bmcl.2009.07.063
53323196 56819 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cncc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643856 56819 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1cncc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
118736623 118970 7 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 267 3 2 3 2.4 CNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425755 118970 7 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 267 3 2 3 2.4 CNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
118733808 120630 0 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3416056 120630 0 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3546908 120630 0 None -1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
44573231 187270 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492911 187270 0 None 5 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
216 2842 32 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
9815618 2842 32 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
CHEMBL253811 2842 32 None 1 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/jm0709034
162653458 183642 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4753812 183642 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802839 183642 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
10331841 169180 6 None -158 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL440752 169180 6 None -158 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1016/j.bmcl.2004.12.080
44412389 78067 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210215 78067 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
162653458 183642 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4753812 183642 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802839 183642 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
11447552 62498 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
CHEMBL178231 62498 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1021/jm0709034
54585653 61435 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 307 2 1 3 2.8 FC(F)(F)c1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770385 61435 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 307 2 1 3 2.8 FC(F)(F)c1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
11427139 84658 0 None -38 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL222566 84658 0 None -38 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
53325937 56775 0 None -53 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643678 56775 0 None -53 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
25070581 61431 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770380 61431 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
134265616 164387 0 None -1548 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4213447 164387 0 None -1548 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
122442286 138326 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138326 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138326 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
118733798 120623 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416051 120623 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546894 120623 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
44573220 187427 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 4 1 3 1.4 CN(CC1CC1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL493951 187427 0 None 4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 4 1 3 1.4 CN(CC1CC1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
162658689 183666 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759181 183666 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803103 183666 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
122442272 138323 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 138323 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 138323 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44572371 12495 0 None -5 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
CHEMBL1186608 12495 0 None -5 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
CHEMBL472678 12495 0 None -5 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1cccc(C#CCCCCO)c1 10.1021/jm801354e
162658689 183666 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4759181 183666 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803103 183666 0 None -28 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
122442272 138323 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 138323 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 138323 0 None -54 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
16115652 83462 0 None -15 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL220211 83462 0 None -15 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
54580776 61432 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770381 61432 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
118736624 118971 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 4 2 3 2.8 CCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425756 118971 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 4 2 3 2.8 CCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
44573229 172652 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc2c(c1)CCNCC2)c1ccccc1F 10.1016/j.bmcl.2009.02.071
CHEMBL449999 172652 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1ccc2c(c1)CCNCC2)c1ccccc1F 10.1016/j.bmcl.2009.02.071
42601405 192630 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 287 2 1 3 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL521805 192630 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 287 2 1 3 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
11221167 84651 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL222514 84651 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
162657053 183657 0 None -20 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4757214 183657 0 None -20 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803017 183657 0 None -20 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
10401602 123043 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL360968 123043 0 None -6 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCOc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
11447552 62498 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL178231 62498 4 None -239 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
25070907 61427 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770376 61427 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
44572369 12426 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186108 12426 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL450178 12426 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 171 2 1 1 1.7 C#Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
46228438 199962 0 None -1862 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595195 199962 0 None -1862 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
45485742 197800 0 None -18 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 318 5 1 5 2.2 Clc1ccccc1CCOc1cncc(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.136
CHEMBL572228 197800 0 None -18 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 318 5 1 5 2.2 Clc1ccccc1CCOc1cncc(N2CCNCC2)n1 10.1016/j.bmcl.2009.07.136
44412405 77752 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209155 77752 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 255 1 1 1 3.4 FC(F)(F)c1cccc([C@H]2CC[C@H]3CNC[C@@H]23)c1 10.1016/j.bmcl.2006.03.007
11777150 62575 0 None -63 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 0 2 2 2.4 CC1CNCCc2cc(O)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178313 62575 0 None -63 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 0 2 2 2.4 CC1CNCCc2cc(O)c(Br)cc21 10.1016/j.bmcl.2004.12.080
11414184 83469 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
CHEMBL220274 83469 0 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
122442324 138325 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138325 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138325 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442324 138325 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770174 138325 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771386 138325 0 None -12 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573216 187314 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 268 4 2 3 1.1 CCCNS(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL493151 187314 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 268 4 2 3 1.1 CCCNS(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
44572759 12430 1 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186135 12430 1 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL451368 12430 1 None -7 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
24773650 154673 2 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
CHEMBL399750 154673 2 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
118733818 120639 0 None -181 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416061 120639 0 None -181 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546956 120639 0 None -181 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
168294162 192987 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5208129 192987 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222770 192987 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
10331841 169180 6 None -158 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
CHEMBL440752 169180 6 None -158 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
168294162 192987 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5208129 192987 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222770 192987 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1ccc(Cl)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
135453290 133581 33 None 1 7 Rat 8.7 pEC50 = 8.7 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133581 33 None 1 7 Rat 8.7 pEC50 = 8.7 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
166 3334 18 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
3045227 3334 18 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
CHEMBL76781 3334 18 None 2 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmc.2007.10.100
36906 104853 75 None 1 3 Rat 8.6 pEC50 = 8.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
CHEMBL31115 104853 75 None 1 3 Rat 8.6 pEC50 = 8.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
44572367 12511 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
CHEMBL1186673 12511 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
CHEMBL474230 12511 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 2 2 2.3 NC[C@H]1C[C@@H]1c1ccccc1C#CCCCCO 10.1021/jm801354e
168291130 192952 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201835 192952 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222548 192952 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168291130 192952 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201835 192952 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222548 192952 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
11290492 137976 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL376456 137976 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
11499800 89078 0 None -10 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337503 89078 0 None -10 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365465 89078 0 None -10 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
122442254 138320 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 138320 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 138320 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442254 138320 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 138320 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 138320 0 None -26 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44572810 12623 2 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL1187196 12623 2 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL493130 12623 2 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
150 2492 21 None -2 17 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
1764 2492 21 None -2 17 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
8226 2492 21 None -2 17 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
CHEMBL1201356 2492 21 None -2 17 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
DB00353 2492 21 None -2 17 Human 7.7 pEC50 = 7.7 Functional
Agonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assayAgonist at human 5HT2B receptor expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
134265663 163655 0 None -19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 243 1 1 3 2.1 c1cc(C2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4204710 163655 0 None -19 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 243 1 1 3 2.1 c1cc(C2CCC2)c2c(n1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
53317923 56816 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
CHEMBL1643853 56816 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1cccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)c1 10.1016/j.bmcl.2010.11.089
53325936 56772 0 None -12 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 335 3 1 6 1.7 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643675 56772 0 None -12 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 335 3 1 6 1.7 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
122442293 138317 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 138317 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 138317 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
122442293 138317 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770599 138317 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771378 138317 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1c(OCCF)ccc(F)c1F 10.1021/acs.jmedchem.5b01153
11658860 2329 51 None -35 11 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
2941 2329 51 None -35 11 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
4374 2329 51 None -35 11 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
CHEMBL360328 2329 51 None -35 11 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
DB04871 2329 51 None -35 11 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
16115381 83414 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL219837 83414 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
44572166 12428 0 None -7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL1186133 12428 0 None -7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL451232 12428 0 None -7 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
118736626 118972 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 307 5 2 3 3.2 c1ccc(Cc2cc3c(c(NCC4CC4)n2)CCNCC3)cc1 10.1021/ml500507v
CHEMBL3425758 118972 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 307 5 2 3 3.2 c1ccc(Cc2cc3c(c(NCC4CC4)n2)CCNCC3)cc1 10.1021/ml500507v
18735305 204910 0 None 2 3 Human 7.7 pEC50 = 7.7 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76301 204910 0 None 2 3 Human 7.7 pEC50 = 7.7 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
54583742 61426 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL1770375 61426 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccccc1Cc1ncc2c(n1)CCNCC2 10.1016/j.bmcl.2010.11.120
44389645 64151 0 None -72 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180867 64151 0 None -72 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
118733790 120645 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416047 120645 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546973 120645 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
44572753 12671 3 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@@H]1C[C@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187565 12671 3 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@@H]1C[C@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL509418 12671 3 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@@H]1C[C@H]1c1ccccc1Br 10.1021/jm801354e
53321947 56768 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 257 1 1 5 1.0 c1cc2nc3c(c(N4CCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643671 56768 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 257 1 1 5 1.0 c1cc2nc3c(c(N4CCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
44431701 88115 0 None 3 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 311 4 1 6 3.4 Cc1noc(Cc2c3ccoc3c(C[C@@H](C)N)c3ccoc23)n1 10.1016/j.bmcl.2007.03.073
CHEMBL234682 88115 0 None 3 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 311 4 1 6 3.4 Cc1noc(Cc2c3ccoc3c(C[C@@H](C)N)c3ccoc23)n1 10.1016/j.bmcl.2007.03.073
44409290 74622 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Efficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPREfficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPR
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203013 74622 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Efficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPREfficacy against human recombinant 5HT2B receptor induced intracellular calcium mobilization in CHO cells by FLIPR
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
10017556 161854 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.5 CC(C)Oc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL415029 161854 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 297 2 1 2 3.5 CC(C)Oc1cc2c(cc1Br)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
118733760 120612 1 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416032 120612 1 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546869 120612 1 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
11630623 89070 0 None -213 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337499 89070 0 None -213 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365399 89070 0 None -213 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
58911653 91087 0 None -25 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397911 91087 0 None -25 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
168291896 192961 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 192961 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 192961 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
145 140 49 None -134 11 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
1832 140 49 None -134 11 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
CHEMBL7257 140 49 None -134 11 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
DB14010 140 49 None -134 11 Rat 6.6 pEC50 = 6.6 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
25070911 111644 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 324 3 1 5 1.6 c1ccc(Cc2nc3c(c(N4CCOCC4)n2)CCNCC3)cc1 10.1021/jm5003292
CHEMBL3286564 111644 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assayAgonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 324 3 1 5 1.6 c1ccc(Cc2nc3c(c(N4CCOCC4)n2)CCNCC3)cc1 10.1021/jm5003292
168291564 192959 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 192959 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 192959 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
168291896 192961 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 192961 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 192961 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442250 138319 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 138319 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 138319 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
5 139 72 None -2 27 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
5202 139 72 None -2 27 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
CHEMBL39 139 72 None -2 27 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
DB08839 139 72 None -2 27 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
168291564 192959 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 192959 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 192959 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
122442250 138319 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 138319 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 138319 0 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
24773816 94827 0 None -31 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL253805 94827 0 None -31 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
24773814 94830 1 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL253809 94830 1 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
11264345 130373 5 None -120 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
CHEMBL368016 130373 5 None -120 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
122442300 138324 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 138324 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 138324 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
122442300 138324 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 138324 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 138324 0 None -8 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
146025684 183611 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 183611 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 183611 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
162652983 183639 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752412 183639 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802814 183639 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
146025684 183611 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4743977 183611 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802486 183611 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 5 1 3 2.2 C=CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
162652983 183639 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752412 183639 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802814 183639 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 247 5 1 3 2.5 CCCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
45484673 198935 0 None -8 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL585012 198935 0 None -8 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
11595191 89031 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337488 89031 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2364960 89031 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
162658153 183661 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4758641 183661 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803076 183661 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
162658153 183661 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4758641 183661 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803076 183661 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 2.5 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
118736627 118973 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 5 2 3 3.2 CCCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425759 118973 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 5 2 3 3.2 CCCNc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
118736631 118976 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 238 2 1 2 2.4 c1ccc(Cc2cc3c(cn2)CCNCC3)cc1 10.1021/ml500507v
CHEMBL3425763 118976 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 238 2 1 2 2.4 c1ccc(Cc2cc3c(cn2)CCNCC3)cc1 10.1021/ml500507v
122442270 138321 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138321 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138321 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442270 138321 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138321 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138321 1 None -6 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11952353 199837 0 None -1905 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
CHEMBL594469 199837 0 None -1905 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
11171955 91064 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
CHEMBL2397888 91064 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
44573002 12654 1 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL1187408 12654 1 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
CHEMBL501854 12654 1 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Br)cc1 10.1021/jm801354e
16115511 84808 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223466 84808 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
162643473 183591 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777303 183591 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802306 183591 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
162643473 183591 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4777303 183591 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802306 183591 0 None -14 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
11300712 141661 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL385577 141661 0 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
44573018 12612 1 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1 10.1021/jm801354e
CHEMBL1187169 12612 1 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1 10.1021/jm801354e
CHEMBL492306 12612 1 None -3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)c(F)c1 10.1021/jm801354e
24826869 91073 0 None -7 3 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397897 91073 0 None -7 3 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
16115654 136949 0 None -46 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374562 136949 0 None -46 3 Human 6.6 pEC50 = 6.6 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
53324629 56769 0 None -4 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 271 1 1 5 1.4 c1cc2nc3c(c(N4CCCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643672 56769 0 None -4 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 271 1 1 5 1.4 c1cc2nc3c(c(N4CCCCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
1355 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
142 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
CHEMBL478 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
DB12110 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
1355 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
142 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
CHEMBL478 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
DB12110 1998 88 None -5 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
46937339 74180 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/ml200206z
CHEMBL2023357 74180 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/ml200206z
46937339 74180 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilizationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilization
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL2023357 74180 0 None -13 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilizationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium mobilization
ChEMBL 235 5 1 2 2.7 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1021/jm5019274
16115392 84768 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223292 84768 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
16115388 137341 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL375302 137341 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
11209786 137215 0 None -208 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375170 137215 0 None -208 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
9859257 205100 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
CHEMBL77880 205100 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
168268877 189946 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189946 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168268877 189946 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189946 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
230 4088 25 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
3045225 4088 25 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
CHEMBL407909 4088 25 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.10.100
5 139 72 None -7 27 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
5202 139 72 None -7 27 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
CHEMBL39 139 72 None -7 27 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
DB08839 139 72 None -7 27 Rat 8.5 pEC50 = 8.5 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
44572798 12618 2 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
CHEMBL1187187 12618 2 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
CHEMBL492926 12618 2 None -1 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1cccc(F)c1 10.1021/jm801354e
46933845 16130 0 None -18 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224034 16130 0 None -18 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor assessed as 5HT-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
54583743 61433 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770382 61433 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
118736630 118975 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 3 1 3 2.4 CN(C)c1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425762 118975 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 281 3 1 3 2.4 CN(C)c1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
122442263 138332 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 138332 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 138332 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44389646 64853 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL182184 64853 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 269 1 1 2 2.7 COc1cc2c(cc1Br)[C@H](C)CNCC2 10.1016/j.bmcl.2004.12.080
122442263 138332 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 138332 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 138332 0 None -30 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442260 138329 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 138329 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 138329 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
11949712 202138 0 None -3019 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL609306 202138 0 None -3019 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
118733764 120619 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416034 120619 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546890 120619 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
118733776 120625 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3416040 120625 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3546903 120625 0 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
70687695 74449 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022186 74449 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027987 74449 0 None -12 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 205 5 1 2 2.5 CCCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
134265675 164343 0 None -40 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
CHEMBL4212834 164343 0 None -40 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 297 2 1 3 2.5 Fc1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
162645074 183600 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4740346 183600 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802388 183600 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
162645074 183600 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4740346 183600 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802388 183600 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 259 5 1 3 3.5 CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
11400855 12422 7 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
CHEMBL1186092 12422 7 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
CHEMBL449134 12422 7 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@@H]1C[C@H]1c1ccccc1 10.1021/jm801354e
57799306 89080 0 None -12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337493 89080 0 None -12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365469 89080 0 None -12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
122442260 138329 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769543 138329 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771390 138329 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44315697 205482 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL80731 205482 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
168268736 192765 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192765 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192765 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
9990808 122746 0 None -51 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1021/jm0709034
CHEMBL360492 122746 0 None -51 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1021/jm0709034
168268736 192765 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192765 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192765 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
11652452 89097 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337492 89097 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365703 89097 0 None -9 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
44572749 12405 1 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL1185954 12405 1 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
CHEMBL443128 12405 1 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccccc1Cl 10.1021/jm801354e
44412150 77704 0 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CCC3CNCC32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL208936 77704 0 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CCC3CNCC32)n1 10.1016/j.bmcl.2006.03.007
11658860 2329 51 None -35 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
2941 2329 51 None -35 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
4374 2329 51 None -35 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
CHEMBL360328 2329 51 None -35 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
DB04871 2329 51 None -35 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
122442250 138319 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 138319 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 138319 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
16115644 136935 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374436 136935 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
118736628 118974 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 4 2 3 3.2 CC(C)Nc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
CHEMBL3425760 118974 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 295 4 2 3 3.2 CC(C)Nc1nc(Cc2ccccc2)cc2c1CCNCC2 10.1021/ml500507v
44573230 187269 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492910 187269 0 None -3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 305 2 1 3 2.3 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
3356430 193022 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5208864 193022 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222941 193022 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
70683433 74429 1 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2022185 74429 1 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
CHEMBL2027895 74429 1 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 191 4 1 2 2.1 CCOc1ccccc1[C@H]1C[C@@H]1CN 10.1021/ml200206z
122442250 138319 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770689 138319 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771380 138319 0 None -8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1cc(F)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442266 138318 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138318 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138318 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442266 138318 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138318 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138318 0 None -51 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573016 12638 1 None -38 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1c(F)cccc1F 10.1021/jm801354e
CHEMBL1187322 12638 1 None -38 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1c(F)cccc1F 10.1021/jm801354e
CHEMBL498863 12638 1 None -38 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1c(F)cccc1F 10.1021/jm801354e
168272608 192769 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192769 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192769 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162657053 183657 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4757214 183657 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803017 183657 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@H]1C[C@@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
168272608 192769 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192769 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192769 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
3356430 193022 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5208864 193022 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222941 193022 2 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44573222 174288 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 2 1 3 1.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCCC1 10.1016/j.bmcl.2009.02.071
CHEMBL455039 174288 0 None 2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 294 2 1 3 1.5 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCCC1 10.1016/j.bmcl.2009.02.071
118733766 120613 0 None -33 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416035 120613 0 None -33 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546870 120613 0 None -33 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 3.2 CCCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
146025686 183735 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4790992 183735 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803813 183735 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
146025686 183735 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4790992 183735 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803813 183735 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 243 5 1 3 3.1 C=CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
44572757 12617 1 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
CHEMBL1187186 12617 1 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
CHEMBL492917 12617 1 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1ccccc1C(F)(F)F 10.1021/jm801354e
45484742 198495 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 243 3 2 3 1.7 c1ccc(COc2n[nH]c3c2CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
CHEMBL577903 198495 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 243 3 2 3 1.7 c1ccc(COc2n[nH]c3c2CCNCC3)cc1 10.1016/j.bmcl.2009.07.063
122442286 138326 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138326 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138326 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442286 138326 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138326 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138326 0 None -34 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
44573221 193056 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 2 1 3 1.2 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCC1 10.1016/j.bmcl.2009.02.071
CHEMBL522514 193056 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 280 2 1 3 1.2 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCCC1 10.1016/j.bmcl.2009.02.071
44622848 193323 0 None -11 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL524778 193323 0 None -11 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 255 2 1 4 1.0 O=c1cc2c(nn1Cc1ccccc1)CCNCC2 10.1016/j.bmcl.2009.07.063
9881119 205450 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
CHEMBL80482 205450 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
9990808 122746 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL360492 122746 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 213 0 1 1 2.7 CC1CNCCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
44573012 12611 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1cccc(F)c1F 10.1021/jm801354e
CHEMBL1187168 12611 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1cccc(F)c1F 10.1021/jm801354e
CHEMBL492305 12611 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1cccc(F)c1F 10.1021/jm801354e
11206703 91063 0 None -12 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397887 91063 0 None -12 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
44572657 12435 6 None -7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL1186169 12435 6 None -7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
CHEMBL452719 12435 6 None -7 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NC[C@H]1C[C@@H]1c1ccccc1 10.1021/jm801354e
44573004 12488 1 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL1186590 12488 1 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
CHEMBL471202 12488 1 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccc([C@H]2C[C@@H]2CN)cc1 10.1021/jm801354e
53325938 56776 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
CHEMBL1643679 56776 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
10105208 62469 0 None -83 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178124 62469 0 None -83 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1016/j.bmcl.2004.12.080
1355 1998 88 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
142 1998 88 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
CHEMBL478 1998 88 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
DB12110 1998 88 None -5 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
24773649 94798 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL253591 94798 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
24773651 154833 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@H](C)CNCC2 10.1021/jm0709034
CHEMBL400600 154833 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@H](C)CNCC2 10.1021/jm0709034
46228437 199961 1 None -39 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595194 199961 1 None -39 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
24773895 94828 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@@H](C)CNCC2 10.1021/jm0709034
CHEMBL253806 94828 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)[C@@H](C)CNCC2 10.1021/jm0709034
122442270 138321 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138321 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138321 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
24773979 130143 21 None -12 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
CHEMBL367796 130143 21 None -12 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
11264955 204938 0 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL76474 204938 0 None 1 3 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
152 363 29 None -2 5 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
2107 363 29 None -2 5 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
CHEMBL275854 363 29 None -2 5 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
11708275 72683 3 None 1 2 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
CHEMBL199775 72683 3 None 1 2 Rat 8.4 pEC50 = 8.4 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
166 3334 18 None 2 4 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
3045227 3334 18 None 2 4 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
CHEMBL76781 3334 18 None 2 4 Human 8.4 pEC50 = 8.4 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
5 139 72 None -2 27 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
5202 139 72 None -2 27 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
CHEMBL39 139 72 None -2 27 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
DB08839 139 72 None -2 27 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF methodAgonist activity at human 5-HT2BR expressed in CHO cells assessed as induction of IP1 accumulation after 30 mins by HTRF method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
16047544 12616 8 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187185 12616 8 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL492916 12616 8 None -3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
44572172 12514 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
CHEMBL1186686 12514 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
CHEMBL474633 12514 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 179 2 1 1 2.2 Cc1cc([C@H]2C[C@@H]2CN)ccc1F 10.1021/jm801354e
16115267 84764 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL223272 84764 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
9994008 166125 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL426235 166125 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 283 2 1 2 3.1 CCC1CNCCc2cc(OC)c(Br)cc21 10.1016/j.bmcl.2004.12.080
122442270 138321 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770753 138321 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771382 138321 1 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
22368315 63736 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 1 1 2 2.1 COc1cc2c(cc1Br)CCNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL180166 63736 0 None -50 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 255 1 1 2 2.1 COc1cc2c(cc1Br)CCNCC2 10.1016/j.bmcl.2004.12.080
134265618 164031 0 None -323 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4209052 164031 0 None -323 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 257 2 1 3 2.1 c1cc(CC2CCC2)c2c(n1)N1CCNCC1CC2 10.1021/acsmedchemlett.8b00328
46884138 8411 0 None -812 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at 5HT2B receptorAgonist activity at 5HT2B receptor
ChEMBL 364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1093699 8411 0 None -812 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at 5HT2B receptorAgonist activity at 5HT2B receptor
ChEMBL 364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
44572812 12482 1 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1 10.1021/jm801354e
CHEMBL1186561 12482 1 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1 10.1021/jm801354e
CHEMBL469729 12482 1 None -5 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1 10.1021/jm801354e
54587669 61430 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
CHEMBL1770379 61430 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 253 2 1 3 2.1 Cc1cccc(Cc2ncc3c(n2)CCNCC3)c1 10.1016/j.bmcl.2010.11.120
11609026 89098 0 None -125 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337500 89098 0 None -125 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365705 89098 0 None -125 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
44573014 12489 1 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
CHEMBL1186595 12489 1 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
CHEMBL471802 12489 1 None -10 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 183 2 1 1 2.0 NC[C@H]1C[C@@H]1c1ccc(F)cc1F 10.1021/jm801354e
3568128 192909 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 192909 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 192909 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
3568128 192909 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 192909 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 192909 1 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
44420682 137583 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
CHEMBL375642 137583 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
118733802 120627 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416053 120627 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546905 120627 0 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
168284548 192887 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5191889 192887 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222143 192887 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
168284548 192887 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5191889 192887 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222143 192887 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 1 3 2 4.1 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
118733788 120638 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416046 120638 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546955 120638 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 237 5 1 2 3.0 C=CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
11658860 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
146025689 183693 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183693 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183693 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
11658860 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
2941 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
4374 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
CHEMBL360328 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
DB04871 2329 51 None -35 11 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.6b01194
146025689 183693 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4781163 183693 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803350 183693 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 271 6 1 3 3.6 C=CCOc1ccc2oc(CC)cc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
118733792 120646 0 None -12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416048 120646 0 None -12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546974 120646 0 None -12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
162659286 183671 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4762225 183671 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803142 183671 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
122442266 138318 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138318 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138318 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442266 138318 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769499 138318 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771379 138318 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.6 C=CCOc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
162659286 183671 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4762225 183671 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803142 183671 0 None -13 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
146025687 183691 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183691 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183691 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
118733804 120628 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3416054 120628 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3546906 120628 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
162668367 183715 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4786831 183715 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803642 183715 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
122442309 138322 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769828 138322 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771383 138322 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
168294156 192981 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5207023 192981 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222736 192981 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
162668367 183715 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4786831 183715 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803642 183715 0 None -21 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.3 CC(C)Oc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
168294156 192981 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5207023 192981 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222736 192981 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442254 138320 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 138320 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 138320 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442309 138322 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769828 138322 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771383 138322 0 None -6 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 5 1 2 2.4 NCC1CC1c1cc(F)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
44572164 12651 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL1187390 12651 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
CHEMBL501526 12651 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1F 10.1021/jm801354e
146025687 183691 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4779260 183691 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4803306 183691 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 249 5 1 3 2.8 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2occc12 10.1021/acs.jmedchem.6b01194
46230099 199289 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590483 199289 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
118733794 120647 0 None -72 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416049 120647 0 None -72 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546975 120647 0 None -72 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 235 4 1 2 2.4 C#CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
122442254 138320 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3770963 138320 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771381 138320 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 213 3 1 2 2.0 COc1ccc(F)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442286 138326 0 None -34 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769987 138326 0 None -34 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771387 138326 0 None -34 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 229 3 1 2 2.6 COc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
45484682 198348 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL576651 198348 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 323 2 1 4 2.0 O=c1cc2c(nn1Cc1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
11658860 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
2941 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
4374 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
CHEMBL360328 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
DB04871 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
44573153 187173 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 336 3 2 3 2.8 O=S(=O)(Nc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492348 187173 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 336 3 2 3 2.8 O=S(=O)(Nc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
44573157 187274 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 316 3 1 3 2.2 CN(c1ccccc1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492950 187274 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 316 3 1 3 2.2 CN(c1ccccc1)S(=O)(=O)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
134265622 164729 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4217787 164729 0 None -81 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 259 1 1 3 2.4 CC(C)(C)Cc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
44412388 78156 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210484 78156 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 272 1 1 4 1.7 C[C@@H]1C[C@H]2CNC[C@H]2N1c1nccc(C(F)(F)F)n1 10.1016/j.bmcl.2006.03.007
145966293 164430 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 267 0 1 3 1.6 Brc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4213971 164430 0 None -14 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 267 0 1 3 1.6 Brc1ccnc2c1CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
18735309 205410 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80246 205410 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
118733814 120632 0 None -23 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3416059 120632 0 None -23 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3546910 120632 0 None -23 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
44572761 12648 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
CHEMBL1187377 12648 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
CHEMBL501117 12648 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1ccccc1O 10.1021/jm801354e
11302765 84219 4 None -309 3 Human 5.3 pEC50 = 5.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL221113 84219 4 None -309 3 Human 5.3 pEC50 = 5.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11448649 83404 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL219734 83404 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
50878551 90716 61 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90716 61 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
50878551 90716 61 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90716 61 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
44572808 12674 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
CHEMBL1187585 12674 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
CHEMBL510383 12674 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 163 2 2 2 1.5 NC[C@H]1C[C@@H]1c1cccc(O)c1 10.1021/jm801354e
44431688 152716 0 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 307 7 1 5 1.6 COCCOCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL397321 152716 0 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 307 7 1 5 1.6 COCCOCc1c2c(c(C[C@@H](C)N)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
5 139 72 None -2 27 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
5202 139 72 None -2 27 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
CHEMBL39 139 72 None -2 27 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
DB08839 139 72 None -2 27 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
135509961 136107 2 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
CHEMBL373245 136107 2 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
9991444 62602 1 None -15 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
CHEMBL178366 62602 1 None -15 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1021/jm0709034
154699445 177402 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
CHEMBL4638592 177402 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
11737032 84987 0 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223896 84987 0 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
162674022 183197 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4796102 183197 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
22292784 64564 15 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
CHEMBL181672 64564 15 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
24773809 94853 0 None -63 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254009 94853 0 None -63 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
122442300 138324 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 138324 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 138324 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
24773900 123406 8 None -6 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1021/jm0709034
CHEMBL361742 123406 8 None -6 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1021/jm0709034
118733778 120634 0 None -19 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3416041 120634 0 None -19 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
CHEMBL3546951 120634 0 None -19 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.2 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC1CC1 10.1021/jm5019274
50942111 56817 0 None -5 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643854 56817 0 None -5 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 365 4 1 7 1.7 COc1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)cc1 10.1016/j.bmcl.2010.11.089
45485725 197804 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.9 C[C@@H](COc1ccccc1Cl)n1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
CHEMBL572252 197804 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.9 C[C@@H](COc1ccccc1Cl)n1nc(N2CCNCC2)ccc1=O 10.1016/j.bmcl.2009.07.136
122442300 138324 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3769421 138324 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771385 138324 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1cc(Cl)c(F)cc1OCCF 10.1021/acs.jmedchem.5b01153
44572698 12520 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
CHEMBL1186700 12520 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
CHEMBL474885 12520 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 197 2 1 1 2.9 NC[C@H]1C[C@@H]1c1ccc2ccccc2c1 10.1021/jm801354e
162652562 183633 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4752604 183633 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 183633 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
11658860 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
2941 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
4374 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
CHEMBL360328 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
DB04871 2329 51 None -35 11 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/acs.jmedchem.5b01153
11666237 89083 0 None -30 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337496 89083 0 None -30 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365472 89083 0 None -30 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
162652562 183633 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4752604 183633 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
CHEMBL4802785 183633 0 None -4 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.3 NC[C@@H]1C[C@H]1c1c(OCC2CC2)ccc2occc12 10.1021/acs.jmedchem.6b01194
44572755 12427 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186115 12427 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL450599 12427 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1ccccc1[C@H]1C[C@@H]1CN 10.1021/jm801354e
22292784 64564 15 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
CHEMBL181672 64564 15 None -17 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1016/j.bmcl.2004.12.080
118733780 120614 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416042 120614 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546871 120614 0 None -7 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 6 1 3 2.4 COCCOc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
3572096 192874 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 192874 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 192874 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
3572096 192874 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 192874 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 192874 1 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
162670523 183726 0 None -20 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4790652 183726 0 None -20 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 183726 0 None -20 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
146025688 183670 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183670 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183670 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
146025688 183670 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4761064 183670 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4803134 183670 0 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 277 6 1 3 3.4 CCc1cc2c([C@H]3C[C@@H]3CN)c(OCCF)ccc2o1 10.1021/acs.jmedchem.6b01194
11313985 91054 0 None -18 3 Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397878 91054 0 None -18 3 Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
11949710 199879 0 None -50 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL594717 199879 0 None -50 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
118733772 120622 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416038 120622 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546893 120622 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
11737939 84198 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL220900 84198 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
11291 3196 26 None 1 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
4980 3196 26 None 1 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
CHEMBL65547 3196 26 None 1 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1016/j.bmcl.2005.06.104
162670523 183726 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4790652 183726 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803766 183726 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
168283046 192868 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 192868 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 192868 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
162676809 183768 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4799299 183768 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804137 183768 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
4240627 192910 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198376 192910 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222297 192910 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
162676809 183768 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4799299 183768 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4804137 183768 0 None -5 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 261 5 1 3 3.4 C=C(F)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
4240627 192910 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198376 192910 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222297 192910 1 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
44431689 87220 0 None -13 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 383 7 1 6 2.6 C[C@@H](N)Cc1c2c(c(COCC(=O)Oc3ccccc3)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL232995 87220 0 None -13 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 383 7 1 6 2.6 C[C@@H](N)Cc1c2c(c(COCC(=O)Oc3ccccc3)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
44572800 12621 3 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL1187194 12621 3 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
CHEMBL493128 12621 3 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 181 2 1 1 2.4 NC[C@H]1C[C@@H]1c1cccc(Cl)c1 10.1021/jm801354e
168283046 192868 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 192868 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 192868 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
44412403 77769 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 222 1 1 2 2.1 Clc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209254 77769 0 None 7 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 222 1 1 2 2.1 Clc1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
135399866 72026 2 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
CHEMBL197653 72026 2 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
44431705 145101 0 None 6 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 313 2 2 4 1.7 C[C@@H](N)[C@H](O)c1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
CHEMBL391196 145101 0 None 6 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HTAgonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT
ChEMBL 313 2 2 4 1.7 C[C@@H](N)[C@H](O)c1c2c(c(Br)c3c1OCC3)OCC2 10.1016/j.bmcl.2007.03.073
18735313 204911 1 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76307 204911 1 None 6 3 Human 8.2 pEC50 = 8.2 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
162650400 183625 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4748110 183625 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802669 183625 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
54581791 61434 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770383 61434 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 273 2 1 3 2.4 Clc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
162650400 183625 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4748110 183625 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
CHEMBL4802669 183625 0 None -22 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 245 4 1 3 3.1 CCc1cc2c([C@H]3C[C@@H]3CN)c(OC)ccc2o1 10.1021/acs.jmedchem.6b01194
53324165 56771 0 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
CHEMBL1643674 56771 0 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 231 2 2 5 0.8 CCNc1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
122442263 138332 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 138332 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 138332 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442263 138332 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769454 138332 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771393 138332 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 245 3 1 2 3.1 COc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
118733800 120626 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416052 120626 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546904 120626 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 251 5 1 2 3.4 C=C(C)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
46230098 199306 0 None -30 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590580 199306 0 None -30 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
134265705 164067 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
CHEMBL4209572 164067 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cnc2c(c1)CC[C@@H]1CNCCN21 10.1021/acsmedchemlett.8b00328
54584721 61428 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770377 61428 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 257 2 1 3 1.9 Fc1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
118733812 120616 0 None -4 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3416058 120616 0 None -4 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
CHEMBL3546873 120616 0 None -4 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 257 6 1 2 3.1 NC[C@@H]1C[C@H]1c1cc(Cl)ccc1OCCCF 10.1021/jm5019274
24849050 78271 2 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
CHEMBL210802 78271 2 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 258 1 1 4 1.3 FC(F)(F)c1ccnc(N2CC[C@H]3CNC[C@H]32)n1 10.1016/j.bmcl.2006.03.007
10036629 64607 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1021/jm0709034
CHEMBL181787 64607 0 None -9 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)C(C)CNCC2 10.1021/jm0709034
24773728 94831 0 None -31 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL253810 94831 0 None -31 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 1 1 1 3.0 CC[C@@H]1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
118733806 120629 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3416055 120629 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
CHEMBL3546907 120629 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 243 5 1 2 2.8 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCCF 10.1021/jm5019274
10064386 63287 4 None -32 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 317 1 1 2 2.5 COc1cc2c(cc1I)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL179378 63287 4 None -32 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 317 1 1 2 2.5 COc1cc2c(cc1I)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
44572802 12412 2 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186019 12412 2 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL445747 12412 2 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
11983273 77967 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
CHEMBL209714 77967 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
ChEMBL 256 1 1 2 2.5 FC(F)(F)c1cccc(N2CC[C@H]3CNC[C@H]32)c1 10.1016/j.bmcl.2006.03.007
118733796 120615 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416050 120615 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546872 120615 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.3 C=C(F)COc1ccc(Cl)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
44572747 12673 2 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
CHEMBL1187580 12673 2 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
CHEMBL510308 12673 2 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccccc1F 10.1021/jm801354e
44573217 187315 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL493152 187315 0 None 10 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
44572174 12515 0 None -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL1186687 12515 0 None -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
CHEMBL474634 12515 0 None -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 195 2 1 1 2.7 Cc1cccc(Cl)c1[C@H]1C[C@@H]1CN 10.1021/jm801354e
44316017 205429 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80366 205429 0 None 4 3 Human 8.1 pEC50 = 8.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
11644842 89068 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337105 89068 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365394 89068 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
53321865 56818 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)nc1 10.1016/j.bmcl.2010.11.089
CHEMBL1643855 56818 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 336 3 1 7 1.1 c1ccc(OC2CN(c3c4c(nc5ccnn35)CCNCC4)C2)nc1 10.1016/j.bmcl.2010.11.089
122442273 138331 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 138331 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 138331 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44316027 205499 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL80862 205499 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
162644827 183599 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4739937 183599 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802378 183599 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
162660358 183680 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762722 183680 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803207 183680 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
122442273 138331 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771152 138331 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771392 138331 0 None -5 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1cc(Cl)c(Cl)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
162644827 183599 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4739937 183599 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4802378 183599 0 None -109 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 217 3 1 3 2.5 COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
53317925 56822 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 390 3 2 7 1.2 O=C1Cc2cc(OC3CN(c4c5c(nc6ccnn46)CCNCC5)C3)ccc2N1 10.1016/j.bmcl.2010.11.089
CHEMBL1643859 56822 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 390 3 2 7 1.2 O=C1Cc2cc(OC3CN(c4c5c(nc6ccnn46)CCNCC5)C3)ccc2N1 10.1016/j.bmcl.2010.11.089
162660358 183680 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4762722 183680 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803207 183680 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 257 5 1 3 3.5 C=C(C)COc1ccc2occc2c1[C@@H]1C[C@H]1CN 10.1021/acs.jmedchem.6b01194
118733816 120633 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416060 120633 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546911 120633 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 223 5 1 2 2.7 CCCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
10624 70271 19 None 6 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
138543650 70271 19 None 6 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL194378 70271 19 None 6 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay
ChEMBL 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
46228422 200013 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595553 200013 0 None -33 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
44572806 12622 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1187195 12622 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL493129 12622 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 177 3 1 2 1.8 COc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
44573218 193033 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 320 3 2 3 2.3 O=S(=O)(Nc1ccccc1F)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL522349 193033 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 320 3 2 3 2.3 O=S(=O)(Nc1ccccc1F)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
1534 103013 53 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103013 53 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103013 53 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
1534 103013 53 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103013 53 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103013 53 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
162659049 183669 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4761526 183669 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803123 183669 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
134265620 164382 0 None -6456 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
CHEMBL4213379 164382 0 None -6456 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 279 2 1 3 2.4 c1ccc(Cc2ccnc3c2CC[C@@H]2CNCCN32)cc1 10.1021/acsmedchemlett.8b00328
162659049 183669 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4761526 183669 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803123 183669 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 219 3 1 3 1.7 COc1ccc2c(c1[C@H]1C[C@@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
44572804 12591 1 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL1187088 12591 1 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
CHEMBL490064 12591 1 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 2.8 NC[C@H]1C[C@@H]1c1cccc(C(F)(F)F)c1 10.1021/jm801354e
162669436 183721 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4789310 183721 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803705 183721 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
134265590 164734 0 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
CHEMBL4217846 164734 0 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2B receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting method
ChEMBL 189 0 1 3 0.8 c1cc2c(cn1)N1CCNC[C@H]1CC2 10.1021/acsmedchemlett.8b00328
9991444 62602 1 None -15 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178366 62602 1 None -15 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2004.12.080
24773900 123406 8 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
CHEMBL361742 123406 8 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 191 1 1 2 1.9 COc1ccc2c(c1)C(C)CNCC2 10.1016/j.bmcl.2004.12.080
162669436 183721 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4789310 183721 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4803705 183721 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 233 4 1 3 2.1 CCOc1ccc2c(c1[C@@H]1C[C@H]1CN)CCO2 10.1021/acs.jmedchem.6b01194
11658860 2329 51 None -35 11 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
2941 2329 51 None -35 11 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
4374 2329 51 None -35 11 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
CHEMBL360328 2329 51 None -35 11 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
DB04871 2329 51 None -35 11 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm0709034
10105208 62469 0 None -83 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL178124 62469 0 None -83 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 CC1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
11160564 63274 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
CHEMBL179337 63274 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1021/jm0709034
23395431 94884 0 None -79 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
CHEMBL254215 94884 0 None -79 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 229 0 1 1 3.0 C[C@@H]1CNCCc2ccc(C(F)(F)F)cc21 10.1021/jm0709034
16115517 84809 0 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL223468 84809 0 None -5 3 Human 8.1 pEC50 = 8.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
44572178 12529 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
CHEMBL1186736 12529 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
CHEMBL475642 12529 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 175 2 1 1 2.4 Cc1cccc([C@H]2C[C@@H]2CN)c1C 10.1021/jm801354e
135520431 72580 9 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL199385 72580 9 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
135414348 72780 2 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
CHEMBL200104 72780 2 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
44573154 187174 0 None -17 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 350 4 2 3 2.5 O=S(=O)(NCc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
CHEMBL492349 187174 0 None -17 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor by cell-based systemAgonist activity at human recombinant 5HT2B receptor by cell-based system
ChEMBL 350 4 2 3 2.5 O=S(=O)(NCc1ccccc1Cl)c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2009.02.071
45484662 198468 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1cccc(Cl)c1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL577691 198468 0 None -2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1cccc(Cl)c1)CCNCC2 10.1016/j.bmcl.2009.07.063
11231392 84865 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223628 84865 0 None -7 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
71682217 91089 0 None -10 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397913 91089 0 None -10 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44572170 12433 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
CHEMBL1186164 12433 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
CHEMBL452458 12433 1 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 215 2 1 1 3.1 NC[C@H]1C[C@@H]1c1ccc(Cl)cc1Cl 10.1021/jm801354e
118733810 120631 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3416057 120631 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
CHEMBL3546909 120631 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 3.0 NC[C@H]1C[C@@H]1c1cc(Cl)ccc1OCC(F)F 10.1021/jm5019274
162657367 183658 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4756903 183658 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 183658 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
45484700 197280 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 295 3 1 4 1.9 O=c1cc2c(nn1Cc1ccc(C3CC3)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL568692 197280 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 295 3 1 4 1.9 O=c1cc2c(nn1Cc1ccc(C3CC3)cc1)CCNCC2 10.1016/j.bmcl.2009.07.063
11160564 63274 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL179337 63274 4 None -40 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 CC1CNCCc2c(Cl)cc(Cl)cc21 10.1016/j.bmcl.2004.12.080
53320653 56770 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 245 2 1 5 0.9 CCN(C)c1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
CHEMBL1643673 56770 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 245 2 1 5 0.9 CCN(C)c1c2c(nc3ccnn13)CCNCC2 10.1016/j.bmcl.2010.11.089
135399666 168739 7 None 1 6 Rat 7.1 pEC50 = 7.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL437314 168739 7 None 1 6 Rat 7.1 pEC50 = 7.1 Functional
Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar ratsActivity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
12370465 12642 18 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL1187354 12642 18 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL500093 12642 18 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
162657367 183658 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4756903 183658 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803034 183658 0 None -32 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 231 4 1 3 2.9 CCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
118733762 120618 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416033 120618 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546889 120618 0 None -6 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 4 1 2 2.8 CCOc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
11437171 83461 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL220207 83461 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2B expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
168286640 192904 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194223 192904 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222252 192904 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168294430 192983 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5205429 192983 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222746 192983 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168294430 192983 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5205429 192983 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222746 192983 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
24826868 91053 1 None 1 3 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397877 91053 1 None 1 3 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayPartial agonist activity at human 5-HT2B receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
11695000 89042 0 None -7 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 89042 0 None -7 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 89042 0 None -7 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
122461343 138337 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 138337 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 138337 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
7153 97992 77 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
CHEMBL272942 97992 77 None 1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O 10.1016/j.bmc.2007.10.100
154699445 177402 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
CHEMBL4638592 177402 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Antagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assayAntagonist activity at human Gq-coupled 5HT2B receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium mobilization by calcium-sensitive dye based FLIPR assay
ChEMBL 319 4 0 4 4.2 CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3)nc2c1 10.1021/acs.jmedchem.0c00807
122461343 138337 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769704 138337 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771398 138337 0 None -9 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(F)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
11514226 89081 0 None -85 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337494 89081 0 None -85 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365470 89081 0 None -85 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2B receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
45484661 198858 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccccc1Cl)CCNCC2 10.1016/j.bmcl.2009.07.063
CHEMBL584210 198858 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2B receptor assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 289 2 1 4 1.6 O=c1cc2c(nn1Cc1ccccc1Cl)CCNCC2 10.1016/j.bmcl.2009.07.063
53325935 56767 0 None -17 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 243 1 1 5 0.6 c1cc2nc3c(c(N4CCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
CHEMBL1643670 56767 0 None -17 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 243 1 1 5 0.6 c1cc2nc3c(c(N4CCC4)n2n1)CCNCC3 10.1016/j.bmcl.2010.11.089
53324630 56773 0 None -18 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
CHEMBL1643676 56773 0 None -18 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2B receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assay
ChEMBL 353 3 1 6 1.8 Fc1ccccc1OC1CN(c2c3c(nc4ccnn24)CCNCC3)C1 10.1016/j.bmcl.2010.11.089
11658860 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
2941 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
4374 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
CHEMBL360328 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
DB04871 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assayAgonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2010.11.120
11658860 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
2941 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
4374 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
CHEMBL360328 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
DB04871 2329 51 None -35 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysisAgonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm5019274
122442275 138336 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 138336 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 138336 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
122442275 138336 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770862 138336 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771397 138336 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(F)c1Cl 10.1021/acs.jmedchem.5b01153
168288743 192923 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 192923 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 192923 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
4543677 192766 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192766 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192766 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
4543677 192766 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192766 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192766 1 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
168288743 192923 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 192923 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 192923 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2B receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
118733774 120624 0 None -10 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416039 120624 0 None -10 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546902 120624 0 None -10 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 4 1 2 3.2 CC(C)Oc1ccc(Cl)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
46228430 199715 0 None -8 3 Human 6.0 pEC50 = 6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL593545 199715 0 None -8 3 Human 6.0 pEC50 = 6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assayAgonist activity against human 5HT2B receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
44138039 179265 10 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473185 179265 10 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565847 180545 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475407 180545 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565831 180412 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475245 180412 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565608 179244 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472990 179244 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
188 3366 80 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
196968 3366 80 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
CHEMBL473186 3366 80 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
44565850 179709 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474408 179709 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
4366334 80380 8 None - 1 Human 8.7 pIC50 = 8.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 379 3 0 4 4.6 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL214554 80380 8 None - 1 Human 8.7 pIC50 = 8.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 379 3 0 4 4.6 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565638 189605 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514934 189605 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3743171 80105 13 None - 1 Human 7.0 pIC50 = 7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL213329 80105 13 None - 1 Human 7.0 pIC50 = 7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
145976085 163641 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204576 163641 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
145972374 164650 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
CHEMBL4216860 164650 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
44565828 179174 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
CHEMBL472416 179174 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
127035063 136461 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
CHEMBL3736149 136461 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
127037093 136483 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736252 136483 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
118464427 138309 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 138309 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
752565 138264 8 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 273 2 3 6 1.7 COc1cccc(NC2=NC(N)=NC3(CCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770770 138264 8 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 273 2 3 6 1.7 COc1cccc(NC2=NC(N)=NC3(CCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
44565849 179271 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 431 5 1 3 4.9 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473235 179271 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 431 5 1 3 4.9 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565805 189610 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514967 189610 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416247 141433 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 393 3 0 4 4.9 CCCN1CCC2(CC1)Oc1ccc(C)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384255 141433 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 393 3 0 4 4.9 CCCN1CCC2(CC1)Oc1ccc(C)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44156863 8046 0 None -21 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091206 8046 0 None -21 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
44565827 179173 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccc2)cn1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472415 179173 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccc2)cn1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565636 179243 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1ccc(-c2ncccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472986 179243 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1ccc(-c2ncccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
16812804 171096 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL445809 171096 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565606 179216 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472789 179216 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565806 180084 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474839 180084 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
168295984 192196 0 None -8 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5204813 192196 0 None -8 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
127034715 136369 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735261 136369 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
127035064 136446 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735911 136446 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
127034730 136414 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735643 136414 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
46830134 8185 0 None -37 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1092241 8185 0 None -37 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
3781561 138573 6 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Br)cc3)CC21 10.1016/j.bmcl.2006.06.068
CHEMBL377562 138573 6 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Br)cc3)CC21 10.1016/j.bmcl.2006.06.068
10449757 3469 35 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
190 3469 35 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
CHEMBL2110371 3469 35 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
71528206 86942 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323581 86942 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
3830738 141621 7 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 2 0 4 5.1 CC(C)N1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL385346 141621 7 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 2 0 4 5.1 CC(C)N1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565831 180412 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475245 180412 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 345 4 1 2 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
145988313 167211 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 167211 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
4203621 138963 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 2 0 5 4.3 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Cl)cc3)CC21 10.1016/j.bmcl.2006.06.068
CHEMBL378541 138963 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 2 0 5 4.3 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(Cl)cc3)CC21 10.1016/j.bmcl.2006.06.068
3898525 139554 8 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 362 3 0 5 3.8 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL379734 139554 8 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 362 3 0 5 3.8 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
44565635 179242 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472985 179242 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565641 179294 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 353 3 1 2 4.5 O=C(c1ccc(-c2ccccc2)cc1)N1CC(c2nc3ccccc3[nH]2)C1 10.1016/j.bmcl.2009.02.126
CHEMBL473391 179294 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 353 3 1 2 4.5 O=C(c1ccc(-c2ccccc2)cc1)N1CC(c2nc3ccccc3[nH]2)C1 10.1016/j.bmcl.2009.02.126
44565829 179194 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 0 3 5.5 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472589 179194 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 0 3 5.5 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2009.02.126
53327611 69725 0 None -154 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69725 0 None -154 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
44416290 141359 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 424 4 0 5 4.7 c1ccc(CCN2CCC3(CC2)Oc2ccccc2C2CC(c4ccncc4)=NN23)cc1 10.1016/j.bmcl.2006.06.068
CHEMBL383860 141359 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 424 4 0 5 4.7 c1ccc(CCN2CCC3(CC2)Oc2ccccc2C2CC(c4ccncc4)=NN23)cc1 10.1016/j.bmcl.2006.06.068
44565824 179269 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473214 179269 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44155109 8142 4 None -21 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091919 8142 4 None -21 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
732268 138271 33 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770837 138271 33 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
44565635 179242 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472985 179242 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2ccccn2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3716424 81021 6 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC(F)F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215380 81021 6 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC(F)F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
3826158 79898 12 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 469 4 0 5 5.2 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212506 79898 12 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 469 4 0 5 5.2 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(OC)cc3)=NN12 10.1016/j.bmcl.2006.06.068
118464428 138236 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 4 3 7 2.6 CCCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770512 138236 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 4 3 7 2.6 CCCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
145988313 167211 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 167211 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assayAntagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced calcium flux preincubated for 60 mins at 37 degC followed by incubation at room temperature for 15 mins and subsequent addition of serotonin and measured for 100 secs in presence of human serum albumin by fluorescence assay
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
136020618 163890 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4207302 163890 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
3736302 138893 7 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 439 2 0 4 5.2 CC(C)N1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL378357 138893 7 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 439 2 0 4 5.2 CC(C)N1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
188 3366 80 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
196968 3366 80 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
CHEMBL473186 3366 80 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2009.02.126
145979048 166634 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 407 3 3 7 3.0 CCOC(=O)c1cc(Br)cc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
CHEMBL4281546 166634 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 407 3 3 7 3.0 CCOC(=O)c1cc(Br)cc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
44565846 180544 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475406 180544 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
16812804 171096 8 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL445809 171096 8 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 3 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565830 179698 2 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474404 179698 2 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565605 189669 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL515422 189669 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416309 141416 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 376 3 0 5 4.1 CC(C)CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384160 141416 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 376 3 0 5 4.1 CC(C)CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
145993660 167345 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 413 1 3 5 3.6 NC1=NC2(CCCCC2)NC(Nc2cc(Br)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4294723 167345 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 413 1 3 5 3.6 NC1=NC2(CCCCC2)NC(Nc2cc(Br)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
44565637 179266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 398 3 2 3 3.9 O=C(c1ccc(-c2ccccc2)[nH]c1=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473187 179266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 398 3 2 3 3.9 O=C(c1ccc(-c2ccccc2)[nH]c1=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
71528204 86940 0 None -15 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323579 86940 0 None -15 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
118464429 167093 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4290245 167093 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
26694436 162888 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 354 5 2 3 2.9 CC(C)NS(=O)(=O)c1cccc(C(=O)Nc2ccc(F)c(F)c2)c1 10.1021/acs.jmedchem.8b00654
CHEMBL4173963 162888 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 354 5 2 3 2.9 CC(C)NS(=O)(=O)c1cccc(C(=O)Nc2ccc(F)c(F)c2)c1 10.1021/acs.jmedchem.8b00654
44565807 180086 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 390 3 1 4 3.4 O=C(c1ccc(N2CCOCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474840 180086 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 390 3 1 4 3.4 O=C(c1ccc(N2CCOCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416259 138178 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 3 0 4 4.7 CCCN1CCC2(CC1)Oc1ccc(F)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL376978 138178 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 397 3 0 4 4.7 CCCN1CCC2(CC1)Oc1ccc(F)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
3649661 138194 7 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 138194 7 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
11502243 189482 48 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
CHEMBL513994 189482 48 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
11949710 199879 0 None -50 3 Human 7.6 pIC50 = 7.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assay relative to 5HTAgonist activity against human 5HT2B receptor by FLIPR assay relative to 5HT
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL594717 199879 0 None -50 3 Human 7.6 pIC50 = 7.6 Functional
Agonist activity against human 5HT2B receptor by FLIPR assay relative to 5HTAgonist activity against human 5HT2B receptor by FLIPR assay relative to 5HT
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
5093797 81044 7 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215461 81044 7 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Cl)cc3)=NN12 10.1016/j.bmcl.2006.06.068
895660 32363 8 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 287 2 3 6 2.0 COc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL1411080 32363 8 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 287 2 3 6 2.0 COc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
118464425 138284 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 138284 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
5113614 80032 7 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 457 3 0 4 5.3 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL213005 80032 7 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 457 3 0 4 5.3 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565808 180887 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL475778 180887 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
11502243 189482 48 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
CHEMBL513994 189482 48 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmcl.2009.02.126
11957541 1446 40 None 1 4 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
1229 1446 40 None 1 4 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
147 1446 40 None 1 4 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
170617 1446 40 None 1 4 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
CHEMBL6616 1446 40 None 1 4 Human 8.5 pIC50 = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
3723094 79935 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 429 1 0 4 4.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212656 79935 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 429 1 0 4 4.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565608 179244 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472990 179244 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 385 4 1 3 3.8 O=S(=O)(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565846 180544 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475406 180544 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 395 4 1 2 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
168284710 191569 0 None -18 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5195241 191569 0 None -18 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2B receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
136020617 57293 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL1651095 57293 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
44565805 189610 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514967 189610 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.6 O=C(c1ccc(C2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44416260 79962 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 413 3 0 4 5.2 CCCN1CCC2(CC1)Oc1ccc(Cl)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212755 79962 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 413 3 0 4 5.2 CCCN1CCC2(CC1)Oc1ccc(Cl)cc1C1CC(c3ccc(F)cc3)=NN12 10.1016/j.bmcl.2006.06.068
44565847 180545 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL475407 180545 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 3 3.6 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565808 180887 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL475778 180887 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 411 4 1 3 5.3 COc1ccc(-c2ccc(C(=O)N3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
11248240 2646 4 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.6b01183
5601 2646 4 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.6b01183
CHEMBL175543 2646 4 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.6b01183
752521 198714 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 198714 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
118464420 138220 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 138220 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
44565634 179217 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2cccnc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472791 179217 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.6 O=C(c1ccc(-c2cccnc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565850 179709 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474408 179709 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 349 3 1 2 4.2 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
118464420 138220 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770342 138220 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
118464426 138221 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 327 4 3 6 3.0 CCCC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770351 138221 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 327 4 3 6 3.0 CCCC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
3751272 80567 13 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 443 3 0 4 5.9 Clc1ccc(C2=NN3C(C2)c2ccccc2OC32CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2006.06.068
CHEMBL215024 80567 13 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 443 3 0 4 5.9 Clc1ccc(C2=NN3C(C2)c2ccccc2OC32CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2006.06.068
71528205 86941 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323580 86941 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection methodAntagonist activity at human 5-HT2B receptor transfected in CHO cell assessed as decrease in 5-HT-induced IP1 production preincubated for 5 mins before 5-HT addition measured after 30 mins by HTRF detection method
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
145963830 164099 0 None 3 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 164099 0 None 3 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
127035065 136475 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
CHEMBL3736207 136475 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
44565606 179216 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472789 179216 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 411 4 1 3 5.3 COc1cc(-c2ccccc2)ccc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
73389570 161978 38 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 378 5 2 4 2.5 Cc1cc(NC(=O)c2cccc(S(=O)(=O)N[C@H]3CCOC3)c2)ccc1F 10.1021/acs.jmedchem.8b00654
CHEMBL4159471 161978 38 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 378 5 2 4 2.5 Cc1cc(NC(=O)c2cccc(S(=O)(=O)N[C@H]3CCOC3)c2)ccc1F 10.1021/acs.jmedchem.8b00654
2884131 166884 7 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4286420 166884 7 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
44155107 8047 4 None -60 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091207 8047 4 None -60 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetryAntagonist activity at human 5HT2B receptor in HEK293 cells assessed as inhibition of alpha-ME-5-HT-induced cAMP accumulation pretreated for 15 secs before alphaME-5-HT addition by Fura-2AM dye based spectrofluorimetry
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
4297073 81272 7 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 348 2 0 5 3.4 CCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215883 81272 7 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 348 2 0 5 3.4 CCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
46933845 16130 0 None -18 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assayAntagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224034 16130 0 None -18 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assayAntagonist activity at human 5HT2B receptor assessed as inhibition of 10633-induced calcium mobilization by FLIPR assay
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
135753059 190694 5 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 4 2 5 2.7 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccc(C)c(C)c2)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5182403 190694 5 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 4 2 5 2.7 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccc(C)c(C)c2)n1 10.1021/acs.jmedchem.1c01759
135753074 191084 9 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5187824 191084 9 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
135753056 191151 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5188949 191151 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
156208582 192009 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 5 2 5 2.6 CCc1cccc(C(=O)Nc2cc(C)nn2-c2nc(CC)cc(=O)[nH]2)c1 10.1021/acs.jmedchem.1c01759
CHEMBL5202029 192009 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assayAntagonist activity at 5-HT2B receptor (unknown origin) transfected in HEK293 cells assessed as beta-arrestin translocation by Tango assay
ChEMBL 351 5 2 5 2.6 CCc1cccc(C(=O)Nc2cc(C)nn2-c2nc(CC)cc(=O)[nH]2)c1 10.1021/acs.jmedchem.1c01759
3765560 141520 9 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384745 141520 9 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
4518239 81028 6 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3OC(F)F)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215404 81028 6 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 477 3 0 5 5.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3OC(F)F)=NN12 10.1016/j.bmcl.2006.06.068
879244 28168 8 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
CHEMBL1373650 28168 8 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
4322819 80394 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 381 2 0 5 3.8 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(F)cc3)CC21 10.1016/j.bmcl.2006.06.068
CHEMBL214594 80394 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 381 2 0 5 3.8 COc1cccc2c1OC1(CCN(C)CC1)N1N=C(c3ccc(F)cc3)CC21 10.1016/j.bmcl.2006.06.068
118464421 167268 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4293638 167268 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
44247568 82145 55 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5HT2B receptorAntagonist activity at human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
CHEMBL2170062 82145 55 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5HT2B receptorAntagonist activity at human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
44565806 180084 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474839 180084 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 388 3 1 3 4.6 O=C(c1ccc(N2CCCCC2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
2267399 138316 8 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 271 1 3 5 2.3 Cc1ccc(NC2=NC(N)=NC3(CCCCC3)N2)cc1 10.1021/acs.jmedchem.5b01631
CHEMBL3771373 138316 8 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 271 1 3 5 2.3 Cc1ccc(NC2=NC(N)=NC3(CCCCC3)N2)cc1 10.1021/acs.jmedchem.5b01631
136928971 138204 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 3 3 7 2.5 CCOC(=O)c1cccc(NC2=NC(NC)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770185 138204 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 343 3 3 7 2.5 CCOC(=O)c1cccc(NC2=NC(NC)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
5128094 79828 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 333 1 0 4 3.7 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212228 79828 18 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 333 1 0 4 3.7 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
5167627 80033 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 3 0 4 5.1 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL213006 80033 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 395 3 0 4 5.1 CCCN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
44416351 80106 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 279 1 0 4 3.4 CC1(C)Oc2ccccc2C2CC(c3ccncc3)=NN21 10.1016/j.bmcl.2006.06.068
CHEMBL213332 80106 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 279 1 0 4 3.4 CC1(C)Oc2ccccc2C2CC(c3ccncc3)=NN21 10.1016/j.bmcl.2006.06.068
3802375 80288 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 453 3 0 4 5.5 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(C)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL214184 80288 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 453 3 0 4 5.5 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(C)cc3)=NN12 10.1016/j.bmcl.2006.06.068
4657811 80490 8 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 461 1 0 4 5.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc4ccccc4c3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL214802 80490 8 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 461 1 0 4 5.6 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc4ccccc4c3)=NN12 10.1016/j.bmcl.2006.06.068
5165122 81022 20 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1 10.1016/j.bmcl.2006.06.068
CHEMBL215386 81022 20 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1 10.1016/j.bmcl.2006.06.068
3757038 81444 11 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 401 1 0 5 4.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccco3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL215991 81444 11 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 401 1 0 5 4.0 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccco3)=NN12 10.1016/j.bmcl.2006.06.068
3773677 138960 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccccc1C1=NN2C(C1)c1cc(Br)ccc1OC21CCN(C)CC1 10.1016/j.bmcl.2006.06.068
CHEMBL378540 138960 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 441 2 0 5 4.4 COc1ccccc1C1=NN2C(C1)c1cc(Br)ccc1OC21CCN(C)CC1 10.1016/j.bmcl.2006.06.068
3410378 141437 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 417 1 0 5 4.5 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3cccs3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384270 141437 7 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 417 1 0 5 4.5 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3cccs3)=NN12 10.1016/j.bmcl.2006.06.068
4679720 165953 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 471 3 0 6 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1OC 10.1016/j.bmcl.2006.06.068
CHEMBL425260 165953 6 None - 1 Human 5.3 pIC50 = 5.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 471 3 0 6 4.4 COc1ccc(C2=NN3C(C2)c2cc(Br)ccc2OC32CCN(C)CC2)cc1OC 10.1016/j.bmcl.2006.06.068
4148445 138276 9 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770873 138276 9 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assayAntagonist activity at 5-HT2B receptor (unknown origin) expressed in CHO-K1 cells assessed as calcium flux after 60 mins by FLIPR assay
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01631
3391669 141816 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 479 1 0 4 5.7 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)c(Cl)c3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL386459 141816 7 None - 1 Human 6.3 pIC50 = 6.3 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 479 1 0 4 5.7 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Cl)c(Cl)c3)=NN12 10.1016/j.bmcl.2006.06.068
44565607 189541 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514453 189541 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565848 179270 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473234 179270 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565826 179172 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.2 O=C(C1CCC(c2ccccc2)CC1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL472414 179172 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 387 3 1 2 5.2 O=C(C1CCC(c2ccccc2)CC1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44476436 82318 6 None -7413 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining methodAntagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining method
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172186 82318 6 None -7413 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining methodAntagonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alphamethyl5HT-induced intracellular calcium mobilization by Fluo4-based staining method
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
162674022 183197 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assayAntagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4796102 183197 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assayAntagonist activity at 5-HT2B receptor (unknown origin) assessed as inhibition of 5HT-indued response by calcium mobilization assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
127037059 136512 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736516 136512 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
10449757 3469 35 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
190 3469 35 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
CHEMBL2110371 3469 35 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10.1016/j.bmcl.2009.02.126
44565639 179293 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL473387 179293 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
44565640 189481 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL513993 189481 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 382 3 1 3 4.2 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44138039 179265 10 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473185 179265 10 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 363 4 1 2 4.3 O=C(c1ccc(-c2ccc(F)cc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565605 189669 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL515422 189669 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 383 3 1 4 4.0 O=C(c1cnc(-c2ccccc2)nc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565639 179293 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
CHEMBL473387 179293 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 367 4 1 2 5.6 c1ccc(-c2ccc(CN3CCC(c4nc5ccccc5[nH]4)CC3)cc2)cc1 10.1016/j.bmcl.2009.02.126
145989393 167199 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 353 1 3 5 2.9 NC1=NC2(CCCCC2)NC(Nc2cc(F)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4292168 167199 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assayAntagonist activity at 5HT2B (unknown origin) expressed in CHOK1 cells assessed as inhibition of agonist-induced effect preincubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent agonist addition measured for 100 secs by fluorescence assay
ChEMBL 353 1 3 5 2.9 NC1=NC2(CCCCC2)NC(Nc2cc(F)cc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
3473601 140104 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL380167 140104 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 367 1 0 4 4.3 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
44565830 179698 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL474404 179698 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 331 3 1 2 4.1 O=C(c1ccc(-c2ccccc2)cc1)N1CCC(c2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
57495353 125014 38 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of 5-HT2B (unknown origin) by calcium flux assayInhibition of 5-HT2B (unknown origin) by calcium flux assay
ChEMBL 450 5 1 7 2.9 CCC(=O)N1CC[C@H](Nc2ncnc3c2CN(c2cnc(OC)c(C(F)(F)F)c2)CC3)C1 10.1021/acsmedchemlett.7b00293
CHEMBL3643413 125014 38 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of 5-HT2B (unknown origin) by calcium flux assayInhibition of 5-HT2B (unknown origin) by calcium flux assay
ChEMBL 450 5 1 7 2.9 CCC(=O)N1CC[C@H](Nc2ncnc3c2CN(c2cnc(OC)c(C(F)(F)F)c2)CC3)C1 10.1021/acsmedchemlett.7b00293
3400827 79884 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 517 3 0 4 6.0 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212457 79884 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 517 3 0 4 6.0 CCCN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccc(Br)cc3)=NN12 10.1016/j.bmcl.2006.06.068
127035062 136426 0 None 6 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 136426 0 None 6 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
127035066 136396 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735434 136396 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assayAntagonist activity at human recombinant 5-HT2B receptor expressed in Flp-In HEK cells in the presence of agonist preincubated for 10 mins by FLIPR based calcium mobilization assay
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
44565828 179174 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
CHEMBL472416 179174 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 395 3 0 3 5.3 Cn1c(C2CCN(C(=O)c3ccc(-c4ccccc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.02.126
145964159 164305 0 None 8 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4212435 164305 0 None 8 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium release assay
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
44565638 189605 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514934 189605 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 417 4 1 3 4.8 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3499360 141495 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL384579 141495 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 445 1 0 4 5.1 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3Cl)=NN12 10.1016/j.bmcl.2006.06.068
104697662 145380 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
CHEMBL3914002 145380 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
11536299 183262 8 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilizationAntagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
CHEMBL479683 183262 8 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilizationAntagonist activity at 5-HT2B receptor (unknown origin) expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
109052212 162523 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 340 4 2 2 4.1 O=C(Nc1ccc(F)cc1)c1cccc(C(=O)NC2CCCCC2)c1 10.1021/acs.jmedchem.8b00654
CHEMBL4168125 162523 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at 5-HT2B (unknown origin)Antagonist activity at 5-HT2B (unknown origin)
ChEMBL 340 4 2 2 4.1 O=C(Nc1ccc(F)cc1)c1cccc(C(=O)NC2CCCCC2)c1 10.1021/acs.jmedchem.8b00654
44565607 189541 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL514453 189541 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 427 5 1 5 4.4 CCOc1nc(-c2ccccc2)ncc1C(=O)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
3442850 169537 20 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL443570 169537 20 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 411 1 0 4 4.4 CN1CCC2(CC1)Oc1ccc(Br)cc1C1CC(c3ccccc3)=NN12 10.1016/j.bmcl.2006.06.068
4895014 79971 7 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 334 1 0 5 3.0 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
CHEMBL212780 79971 7 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium releaseActivity at 5HT2B receptor expressed in CHO cell assessed as inhibition of alpha-methyl-5HT-stimulated calcium release
ChEMBL 334 1 0 5 3.0 CN1CCC2(CC1)Oc1ccccc1C1CC(c3ccncc3)=NN12 10.1016/j.bmcl.2006.06.068
44565824 179269 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473214 179269 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assayAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
ChEMBL 465 4 1 3 6.1 O=C(c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)N1CCC(c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2009.02.126
44565848 179270 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
CHEMBL473234 179270 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albuminAntagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
ChEMBL 381 5 1 3 3.7 O=S(=O)(c1ccc(-c2ccccc2)cc1)N1CCC(Cc2ncc[nH]2)CC1 10.1016/j.bmcl.2009.02.126
12611598 60407 6 None - 0 Rat 7.0 pKd = 7 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
CHEMBL175205 60407 6 None - 0 Rat 7.0 pKd = 7 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
221 3465 71 None - 3 Rat 8.0 pKd = 8.0 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 10.1021/jm00006a001
3277600 3465 71 None - 3 Rat 8.0 pKd = 8.0 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 10.1021/jm00006a001
CHEMBL323356 3465 71 None - 3 Rat 8.0 pKd = 8.0 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 10.1021/jm00006a001
44385952 62178 5 None - 0 Rat 7.9 pKd = 7.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
CHEMBL177800 62178 5 None - 0 Rat 7.9 pKd = 7.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
135398737 955 93 None - 43 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
38 955 93 None - 43 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
722 955 93 None - 43 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
CHEMBL42 955 93 None - 43 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
DB00363 955 93 None - 43 Rat 6.9 pKd = 6.9 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
10022745 119943 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 381 5 1 4 3.5 CCc1c(C)[nH]c2c1C(=O)CC(CN1CCN(c3ccccc3OC)CC1)C2 10.1021/jm011014y
CHEMBL349832 119943 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 381 5 1 4 3.5 CCc1c(C)[nH]c2c1C(=O)CC(CN1CCN(c3ccccc3OC)CC1)C2 10.1021/jm011014y
44327167 9346 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL111393 9346 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL544319 9346 0 None - 0 Rat 6.9 pKd = 6.9 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm011014y
12611606 60348 9 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
CHEMBL174723 60348 9 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
12611609 60406 6 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
CHEMBL175204 60406 6 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
12611617 60325 3 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174563 60325 3 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
12611598 60407 6 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
CHEMBL175205 60407 6 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(O)c(CC(C)N)c1 10.1021/jm00183a006
10356829 59661 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 289 2 2 4 4.3 Cc1cc(NC(=O)Nc2ccc3sccc3c2)sn1 10.1021/jm00006a001
CHEMBL172269 59661 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 289 2 2 4 4.3 Cc1cc(NC(=O)Nc2ccc3sccc3c2)sn1 10.1021/jm00006a001
10693836 9305 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL111189 9305 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL545488 9305 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
10715378 15486 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 389 4 1 4 3.7 COc1ccccc1N1CCN(CC2CC(=O)c3c([nH]c4ccccc34)C2)CC1 10.1021/jm011014y
CHEMBL121744 15486 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 389 4 1 4 3.7 COc1ccccc1N1CCN(CC2CC(=O)c3c([nH]c4ccccc34)C2)CC1 10.1021/jm011014y
9979654 207896 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL96781 207896 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
12611613 60430 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
CHEMBL175328 60430 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
10473483 8618 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 356 4 0 5 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccsc3C2)CC1 10.1021/jm011014y
CHEMBL109528 8618 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 356 4 0 5 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccsc3C2)CC1 10.1021/jm011014y
CHEMBL544318 8618 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 356 4 0 5 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccsc3C2)CC1 10.1021/jm011014y
135398737 955 93 None - 43 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
38 955 93 None - 43 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
722 955 93 None - 43 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
CHEMBL42 955 93 None - 43 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
DB00363 955 93 None - 43 Rat 6.8 pKd = 6.8 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm011014y
10710246 121101 0 None - 0 Rat 5.7 pKd = 5.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL357517 121101 0 None - 0 Rat 5.7 pKd = 5.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm0009890
10338282 34657 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptor
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143022 34657 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B) receptor
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
10338282 34657 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL143022 34657 1 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm011014y
11760018 53335 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 354 5 0 5 3.2 COc1ccccc1N1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
CHEMBL160019 53335 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 354 5 0 5 3.2 COc1ccccc1N1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
44326982 8627 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm011014y
CHEMBL109548 8627 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm011014y
CHEMBL545727 8627 0 None - 0 Rat 6.7 pKd = 6.7 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm011014y
10090486 53242 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 369 5 0 4 4.1 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
CHEMBL159929 53242 0 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 369 5 0 4 4.1 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3occc3C2=O)CC1 10.1021/jm011014y
10090424 34667 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143027 34667 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
10090424 34667 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL143027 34667 1 None - 0 Rat 6.6 pKd = 6.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm011014y
12611604 60417 4 None - 0 Rat 5.6 pKd = 5.6 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)c(O)c1 10.1021/jm00183a006
CHEMBL175272 60417 4 None - 0 Rat 5.6 pKd = 5.6 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)c(O)c1 10.1021/jm00183a006
10645469 110530 0 None - 0 Rat 5.6 pKd = 5.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL325253 110530 0 None - 0 Rat 5.6 pKd = 5.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL542428 110530 0 None - 0 Rat 5.6 pKd = 5.6 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
12611615 60305 1 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174449 60305 1 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
12611617 60325 3 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174563 60325 3 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 4 1 3 1.5 COc1ccc(O)c(CCN(C)C)c1 10.1021/jm00183a006
10024430 207590 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL95098 207590 0 None - 0 Rat 7.5 pKd = 7.5 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
12611613 60430 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
CHEMBL175328 60430 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 209 4 1 3 1.9 COc1ccc(O)c(CC(C)N(C)C)c1 10.1021/jm00183a006
44327153 109183 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determinedAntagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determined
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm011014y
CHEMBL321682 109183 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determinedAntagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determined
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm011014y
CHEMBL558817 109183 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determinedAntagonistic activity on 5-hydroxytryptamine 2B receptor of Rat stomach fundus;ND is not determined
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm011014y
10804995 35551 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143937 35551 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm0009890
10804995 35551 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL143937 35551 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 311 3 0 5 2.2 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2occc21 10.1021/jm011014y
197139 25040 26 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
CHEMBL1347 25040 26 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
12611606 60348 9 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
CHEMBL174723 60348 9 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 181 3 2 3 1.3 COc1ccc(CC(C)N)cc1O 10.1021/jm00183a006
12611596 60274 6 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
CHEMBL174380 60274 6 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
12611615 60305 1 None - 0 Rat 5.4 pKd = 5.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
CHEMBL174449 60305 1 None - 0 Rat 5.4 pKd = 5.4 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 285 7 0 3 3.4 COc1ccc(OCc2ccccc2)c(CCN(C)C)c1 10.1021/jm00183a006
9951008 206374 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87717 206374 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm011014y
126769 206019 42 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00006a001
CHEMBL536255 206019 42 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00006a001
CHEMBL85194 206019 42 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00006a001
9930475 206267 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87026 206267 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm011014y
10597019 34237 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
CHEMBL142668 34237 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
10597019 34237 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL142668 34237 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 7 0 5 3.4 O=C(CCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
10249506 8773 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL109673 8773 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL544091 8773 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
11141324 53063 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 307 3 0 4 2.6 O=C1CC(CN2CCN(c3ccccn3)CC2)c2ccccc21 10.1021/jm011014y
CHEMBL159771 53063 0 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 307 3 0 4 2.6 O=C1CC(CN2CCN(c3ccccn3)CC2)c2ccccc21 10.1021/jm011014y
9866660 114395 2 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 417 3 1 4 5.1 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
CHEMBL333174 114395 2 None - 0 Rat 6.4 pKd = 6.4 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 417 3 1 4 5.1 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
10061837 120714 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 273 2 2 4 3.8 Cc1cc(NC(=O)Nc2ccc3sccc3c2)on1 10.1021/jm00006a001
CHEMBL354951 120714 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 273 2 2 4 3.8 Cc1cc(NC(=O)Nc2ccc3sccc3c2)on1 10.1021/jm00006a001
10022781 57024 0 None - 0 Rat 6.3 pKd = 6.3 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 382 4 0 5 4.6 O=C1c2ccoc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
CHEMBL164471 57024 0 None - 0 Rat 6.3 pKd = 6.3 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 382 4 0 5 4.6 O=C1c2ccoc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
44326751 108588 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL320572 108588 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL539544 108588 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm011014y
10693017 33807 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
CHEMBL142316 33807 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm0009890
10367486 9262 1 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
CHEMBL110948 9262 1 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
CHEMBL543613 9262 1 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm011014y
10693017 33807 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL142316 33807 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 412 8 0 5 3.8 O=C(CCCCN1CCN(CC2CC(=O)c3ccoc3C2)CC1)c1ccc(F)cc1 10.1021/jm011014y
10069784 14951 1 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 404 4 1 3 4.6 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
CHEMBL120903 14951 1 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 404 4 1 3 4.6 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2[nH]c3ccccc3c21 10.1021/jm011014y
15021876 103383 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm011014y
CHEMBL308480 103383 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm011014y
10809188 9243 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL110847 9243 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL540822 9243 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm011014y
10497359 121711 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm0009890
CHEMBL358895 121711 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptorCompound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm0009890
10497359 121711 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm011014y
CHEMBL358895 121711 0 None - 0 Rat 6.2 pKd = 6.2 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 340 4 0 5 2.9 COc1ccccc1N1CCN(CC2CC(=O)c3ccoc3C2)CC1 10.1021/jm011014y
197139 25040 26 None - 0 Rat 5.2 pKd = 5.2 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
CHEMBL1347 25040 26 None - 0 Rat 5.2 pKd = 5.2 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 181 3 2 3 1.3 COc1cc(CC(C)N)ccc1O 10.1021/jm00183a006
11023903 52725 0 None - 0 Rat 5.2 pKd = 5.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 327 3 0 5 2.7 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2sccc21 10.1021/jm011014y
CHEMBL159466 52725 0 None - 0 Rat 5.2 pKd = 5.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 327 3 0 5 2.7 O=C1CC(CN2CCN(c3ccccn3)CC2)Cc2sccc21 10.1021/jm011014y
10015954 165215 1 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 270 2 2 4 3.1 Cc1cc(NC(=O)Nc2ccc3c(ccn3C)c2)on1 10.1021/jm00006a001
CHEMBL422923 165215 1 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundusAntagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus
ChEMBL 270 2 2 4 3.1 Cc1cc(NC(=O)Nc2ccc3c(ccn3C)c2)on1 10.1021/jm00006a001
9886130 206407 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87943 206407 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
10622347 54374 0 None - 0 Rat 5.1 pKd = 5.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 426 8 0 4 4.0 O=C(CCCN1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
CHEMBL160907 54374 0 None - 0 Rat 5.1 pKd = 5.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 426 8 0 4 4.0 O=C(CCCN1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm011014y
10044334 207098 18 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
CHEMBL92145 207098 18 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm011014y
12611596 60274 6 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
CHEMBL174380 60274 6 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(CC(C)N)c(O)cc1C 10.1021/jm00183a006
44385952 62178 5 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
CHEMBL177800 62178 5 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic against 5-hydroxytryptamine 2B receptorAntagonistic against 5-hydroxytryptamine 2B receptor
ChEMBL 195 3 2 3 1.6 COc1cc(C)c(O)cc1CC(C)N 10.1021/jm00183a006
9951964 206335 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm011014y
CHEMBL87458 206335 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm011014y
12611609 60406 6 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
CHEMBL175204 60406 6 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparationAntagonistic activity against 5-hydroxytryptamine 2B receptor obtained from rat stomach fundus preparation
ChEMBL 167 3 2 3 0.9 COc1ccc(O)c(CCN)c1 10.1021/jm00183a006
2148 3859 114 None - 6 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
2150 3859 114 None - 6 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
2784 3859 114 None - 6 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
5610 3859 114 None - 6 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
CHEMBL11608 3859 114 None - 6 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
DB08841 3859 114 None - 6 Rat 5.1 pKd = 5.1 Functional
Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptorAntagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor
ChEMBL 137 2 2 2 0.9 NCCc1ccc(cc1)O 10.1021/jm00183a006
10022123 53286 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL159969 53286 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm011014y
CHEMBL92673 53286 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm011014y
10544858 170004 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm011014y
CHEMBL444269 170004 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm011014y
CHEMBL542181 170004 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm011014y
11121409 56372 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 341 4 0 5 3.1 O=C1c2ccsc2CCC1CCN1CCN(c2ccccn2)CC1 10.1021/jm011014y
CHEMBL163180 56372 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 341 4 0 5 3.1 O=C1c2ccsc2CCC1CCN1CCN(c2ccccn2)CC1 10.1021/jm011014y
10710246 121101 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm011014y
CHEMBL357517 121101 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundusNegative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
ChEMBL 312 3 0 6 1.6 O=C1CC(CN2CCN(c3ncccn3)CC2)Cc2occc21 10.1021/jm011014y
10017554 4309 29 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandAntagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
CHEMBL101008 4309 29 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandAntagonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
10017554 4309 29 None - 0 Human 8.8 pKi = 8.8 Functional
Agonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligandAgonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
CHEMBL101008 4309 29 None - 0 Human 8.8 pKi = 8.8 Functional
Agonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligandAgonistic activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]-5-HT as radioligand
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm960199j
134143752 150625 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3955519 150625 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
49836525 18775 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278202 18775 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836524 18774 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 2 1 2 4.0 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278201 18774 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 2 1 2 4.0 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
46933091 15731 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222695 15731 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49836526 18616 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 3 1 2 4.4 O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1276859 18616 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 3 1 2 4.4 O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836411 18693 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 3 1 2 4.8 O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277585 18693 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 3 1 2 4.8 O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
44516817 57633 5 None -1023 2 Human 6.0 pKi = 6.0 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilizationAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57633 5 None -1023 2 Human 6.0 pKi = 6.0 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilizationAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
185 3975 60 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
5311271 3975 60 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
CHEMBL74355 3975 60 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
DB16351 3975 60 None - 1 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
49836412 18692 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277584 18692 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836294 18747 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 387 2 0 3 4.4 COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278020 18747 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 387 2 0 3 4.4 COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836522 18763 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 376 2 2 3 3.0 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1 10.1021/jm100856p
CHEMBL1278113 18763 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 376 2 2 3 3.0 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1 10.1021/jm100856p
52944115 18766 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 291 1 0 1 4.2 CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
CHEMBL1278116 18766 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 291 1 0 1 4.2 CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
49833883 15729 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 394 4 1 5 3.1 Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222693 15729 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 394 4 1 5 3.1 Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
44156754 6478 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082763 6478 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
49836299 18712 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277770 18712 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49833886 15746 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 396 5 1 6 2.5 COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222764 15746 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 396 5 1 6 2.5 COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
49836639 18652 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277216 18652 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
46933089 15701 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.5 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222554 15701 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.5 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
46867519 6476 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082761 6476 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
44156752 6548 4 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083075 6548 4 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
10609802 107165 2 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
CHEMBL316527 107165 2 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
155531067 171595 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4465512 171595 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
134141831 146662 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3923870 146662 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
49833882 15728 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222692 15728 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
46933090 15744 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222762 15744 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49836635 18635 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 359 2 1 2 4.0 O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277035 18635 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 359 2 1 2 4.0 O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836409 18704 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 391 2 2 3 3.5 O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277679 18704 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 391 2 2 3 3.5 O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49836300 18711 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 2 1 2 4.8 CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277769 18711 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 389 2 1 2 4.8 CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
134154065 152337 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3970041 152337 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
11957541 1446 40 None 1 4 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
1229 1446 40 None 1 4 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
147 1446 40 None 1 4 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
170617 1446 40 None 1 4 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
CHEMBL6616 1446 40 None 1 4 Human 8.5 pKi = 8.5 Functional
Displacement of radiolabeled DOI from human 5HT2B receptor agonist siteDisplacement of radiolabeled DOI from human 5HT2B receptor agonist site
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm8007618
10609802 107165 2 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
CHEMBL316527 107165 2 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 235 3 1 4 1.1 COc1c2c(c(CCN)c3c1OCC3)CCO2 10.1021/jm970219x
1530 2169 50 None -3 25 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
3827 2169 50 None -3 25 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
7206 2169 50 None -3 25 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
CHEMBL534 2169 50 None -3 25 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
DB00920 2169 50 None -3 25 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
10440 2662 20 None - 3 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2662 20 None - 3 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2662 20 None - 3 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
10751567 4507 3 None - 1 Human 6.5 pKi = 6.5 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
CHEMBL102347 4507 3 None - 1 Human 6.5 pKi = 6.5 Functional
Antagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligandAntagonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
49864841 15699 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
CHEMBL1222552 15699 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
49834053 15745 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 384 4 1 5 2.6 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222763 15745 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 384 4 1 5 2.6 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49836634 18634 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 3 1 2 4.0 O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277034 18634 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 361 3 1 2 4.0 O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49833882 15728 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222692 15728 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
25110703 189696 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL515624 189696 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at 5HT2B receptorAntagonist activity at 5HT2B receptor
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
49836528 18626 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
CHEMBL1276947 18626 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
134152052 153059 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3976121 153059 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assayAntagonist activity at human 5-HT2BR expressed in Flp-In HEK cells assessed as inhibition of 5-HT-induced calcium mobilization preincubated for 5 to 10 mins followed 5-HT addition by Fluo-4 dye based FLIPR assay
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
44156628 6682 4 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083654 6682 4 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometryAntagonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as inhibition of alpha-Me-serotonin-induced intracellular calcium mobilization by spectrophotometry
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
10751567 4507 3 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
CHEMBL102347 4507 3 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 223 4 1 4 1.1 COc1cc(CCN)c2c(c1OC)OCC2 10.1021/jm970219x
38240 107972 22 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 225 6 1 4 1.6 CCOc1c(OC)cc(CCN)cc1OC 10.1021/jm970219x
CHEMBL319415 107972 22 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 225 6 1 4 1.6 CCOc1c(OC)cc(CCN)cc1OC 10.1021/jm970219x
49833884 15730 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 380 4 1 5 2.8 Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2 10.1016/j.bmcl.2010.07.029
CHEMBL1222694 15730 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 380 4 1 5 2.8 Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2 10.1016/j.bmcl.2010.07.029
49864886 15713 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.6 CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222624 15713 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assayAntagonist activity at human 5HT2B receptor expressed in human SHSY5Y cells by FLPR assay
ChEMBL 366 4 1 5 2.6 CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O 10.1016/j.bmcl.2010.07.029
155558626 174737 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4561016 174737 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assayAntagonist activity at human 5HT2B receptor expressed in Flp-In-HEK cells co-expressing Gq assessed as inhibition of 5HT-induced stimulation of calcium mobilization preincubated for 10 mins followed by 5HT addition by fluo-4 calcium dye-based FLIPR assay
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
49836633 18627 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1276948 18627 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
25184832 18663 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277312 18663 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assayAntagonist activity at human 5HT2B receptor expressed in human SH-SY5Y cells by FLIPR assay
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
13139 2474 29 None - 2 Human 6.1 pKi = 6.1 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN 10.1021/jm970219x
4076 2474 29 None - 2 Human 6.1 pKi = 6.1 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN 10.1021/jm970219x
CHEMBL26687 2474 29 None - 2 Human 6.1 pKi = 6.1 Functional
Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligandAgonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand
ChEMBL 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN 10.1021/jm970219x
2995 204382 53 None -154 18 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204382 53 None -154 18 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204382 53 None -154 18 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
1225 1459 26 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1459 26 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1459 26 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1459 26 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1459 26 None -3 11 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
2105 3032 37 None -3 25 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3032 37 None -3 25 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3032 37 None -3 25 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3032 37 None -3 25 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3032 37 None -3 25 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
439280 119993 107 None -25 9 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
Drug Central 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O None
6971044 119993 107 None -25 9 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
Drug Central 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O None
CHEMBL350221 119993 107 None -25 9 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
Drug Central 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O None
11658860 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
2941 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
4374 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
CHEMBL360328 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
DB04871 2329 51 None -35 11 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
30699 217676 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
5215 168943 102 None 1 3 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 250 3 2 5 0.9 Nc1ccc(S(=O)(=O)Nc2ncccn2)cc1 None
CHEMBL439 168943 102 None 1 3 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 250 3 2 5 0.9 Nc1ccc(S(=O)(=O)Nc2ncccn2)cc1 None
4421 217689 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 232 2 1 4 1.4 CCN1C=C(C(O)=O)C(=O)C2=CC=C(C)N=C12 None
14052 172554 51 None 1 5 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 204 9 4 4 -0.3 CC[C@@H](CO)NCCN[C@@H](CC)CO None
CHEMBL44884 172554 51 None 1 5 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 204 9 4 4 -0.3 CC[C@@H](CO)NCCN[C@@H](CC)CO None
33613 217668 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 365 4 4 6 0.0 CC1(C)S[C@@H]2[C@H](NC(=O)[C@H](N)C3=CC=C(O)C=C3)C(=O)N2[C@H]1C(O)=O None
2337 3232 77 None -11 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 None -11 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 None -11 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 None -11 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 None -11 29 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
2585 800 103 None -18 22 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 800 103 None -18 22 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 800 103 None -18 22 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 800 103 None -18 22 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 800 103 None -18 22 Human 8.0 pAC50 = 8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
1343 1876 62 None -14 9 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 1876 62 None -14 9 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 1876 62 None -14 9 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 1876 62 None -14 9 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 1876 62 None -14 9 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
54477 84624 36 None - 23 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
CHEMBL22242 84624 36 None - 23 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1038/s41467-023-40064-9
43815 186896 64 None -1995 25 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 186896 64 None -1995 25 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 186896 64 None -1995 25 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
1353 1898 93 None -295 86 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1898 93 None -295 86 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1898 93 None -295 86 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1898 93 None -295 86 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1898 93 None -295 86 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
2247 504 81 None -4 42 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 504 81 None -4 42 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 504 81 None -4 42 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 504 81 None -4 42 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 504 81 None -4 42 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
4034 55792 55 None - 1 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55792 55 None - 1 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
43815 186896 64 None -1995 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 186896 64 None -1995 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 186896 64 None -1995 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
2435 3563 83 None -2 49 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3563 83 None -2 49 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3563 83 None -2 49 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3563 83 None -2 49 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3563 83 None -2 49 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
1830 2572 44 None - 28 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 2572 44 None - 28 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 2572 44 None - 28 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 2572 44 None - 28 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 2572 44 None - 28 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
2393 3309 82 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
5078 3309 82 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
51 3309 82 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
CHEMBL905 3309 82 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
DB00953 3309 82 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
1605 2327 117 None -1 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
3957 2327 117 None -1 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
7216 2327 117 None -1 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
CHEMBL998 2327 117 None -1 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
DB00455 2327 117 None -1 4 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
228 444 28 None -5 24 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 444 28 None -5 24 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 444 28 None -5 24 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 444 28 None -5 24 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 444 28 None -5 24 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
2865 4112 73 None -12 54 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4112 73 None -12 54 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4112 73 None -12 54 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4112 73 None -12 54 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4112 73 None -12 54 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
3547 141348 71 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL38380 141348 71 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL541388 141348 71 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
5210 33308 48 None -123 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
CHEMBL1200765 33308 48 None -123 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
CHEMBL1419 33308 48 None -123 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 10.1038/s41467-023-40064-9
1343 1876 62 None -14 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 1876 62 None -14 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 1876 62 None -14 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 1876 62 None -14 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 1876 62 None -14 9 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
2402 3345 62 None -9 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095 3345 62 None -9 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
7295 3345 62 None -9 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
CHEMBL589 3345 62 None -9 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
DB00268 3345 62 None -9 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
1201549 594 24 None -26 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 594 24 None -26 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 594 24 None -26 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 594 24 None -26 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 594 24 None -26 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 594 24 None -26 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4199 98817 42 None - 1 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 298 5 1 5 2.2 Cc1cc(-c2ccccc2)nnc1NCCN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL278819 98817 42 None - 1 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 298 5 1 5 2.2 Cc1cc(-c2ccccc2)nnc1NCCN1CCOCC1 10.1038/s41467-023-40064-9
5311507 194792 41 None - 1 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL53904 194792 41 None - 1 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
37 775 60 None 1 17 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 775 60 None 1 17 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 775 60 None 1 17 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 775 60 None 1 17 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 775 60 None 1 17 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
3158 56237 27 None -389 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56237 27 None -389 20 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
2543 3681 68 None -2818 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
5358 3681 68 None -2818 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
54 3681 68 None -2818 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
CHEMBL128 3681 68 None -2818 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
DB00669 3681 68 None -2818 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1038/s41467-023-40064-9
5411 204010 89 None - 2 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL698 204010 89 None - 2 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
3658 4076 53 None - 8 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 4076 53 None - 8 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 4076 53 None - 8 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 4076 53 None - 8 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 4076 53 None - 8 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
1400 1944 70 None - 3 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1944 70 None - 3 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1944 70 None - 3 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1944 70 None - 3 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1944 70 None - 3 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1944 70 None - 3 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
5329102 194703 86 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194703 86 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
1971 2846 38 None -4 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2846 38 None -4 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2846 38 None -4 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2846 38 None -4 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2846 38 None -4 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
1613 2333 53 None - 45 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2333 53 None - 45 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2333 53 None - 45 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2333 53 None - 45 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2333 53 None - 45 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2351 3261 64 None -7 21 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
2820 3261 64 None -7 21 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
5035 3261 64 None -7 21 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
CHEMBL81 3261 64 None -7 21 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
DB00481 3261 64 None -7 21 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
1357 2468 139 None -3890 9 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1038/s41467-023-40064-9
1672 2468 139 None -3890 9 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1038/s41467-023-40064-9
224 2468 139 None -3890 9 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1038/s41467-023-40064-9
896 2468 139 None -3890 9 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1038/s41467-023-40064-9
CHEMBL45 2468 139 None -3890 9 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1038/s41467-023-40064-9
DB01065 2468 139 None -3890 9 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1038/s41467-023-40064-9
119570 3137 96 None -7585 40 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
2233 3137 96 None -7585 40 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
953 3137 96 None -7585 40 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
CHEMBL301265 3137 96 None -7585 40 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
DB00413 3137 96 None -7585 40 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
176 397 66 None -1 31 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 397 66 None -1 31 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 397 66 None -1 31 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 397 66 None -1 31 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 397 66 None -1 31 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
240 941 43 None -6 25 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
2769 941 43 None -6 25 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
44279790 941 43 None -6 25 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
660 941 43 None -6 25 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL1729 941 43 None -6 25 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL560739 941 43 None -6 25 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
DB00604 941 43 None -6 25 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
2284 3160 33 None -16 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3160 33 None -16 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3160 33 None -16 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3160 33 None -16 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3160 33 None -16 29 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
5280343 188251 124 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1038/s41467-023-40064-9
CHEMBL1520590 188251 124 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1038/s41467-023-40064-9
CHEMBL50 188251 124 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1038/s41467-023-40064-9
10831 116937 25 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL338667 116937 25 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
68867 78144 38 None - 0 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL2104523 78144 38 None - 0 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
134 2497 24 None -2 68 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 2497 24 None -2 68 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 2497 24 None -2 68 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 2497 24 None -2 68 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 2497 24 None -2 68 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
2105 3032 37 None -28 33 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 3032 37 None -28 33 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 3032 37 None -28 33 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 3032 37 None -28 33 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 3032 37 None -28 33 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
135409453 3744 41 None 2 2 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3744 41 None 2 2 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3744 41 None 2 2 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
20628 96519 28 None - 0 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
CHEMBL26291 96519 28 None - 0 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
441074 19382 82 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL1294 19382 82 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
165193 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
2303 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4946 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
564 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
62882 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
63 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
66366 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
91536 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL27 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL452861 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
DB00571 3165 68 None -72 43 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
135398745 2893 112 None -5 66 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2893 112 None -5 66 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2893 112 None -5 66 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2893 112 None -5 66 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
103 4122 61 None 1 54 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4122 61 None 1 54 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4122 61 None 1 54 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4122 61 None 1 54 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4122 61 None 1 54 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5666 102965 35 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 237 5 1 4 1.5 CCOc1ccccc1OCC1CNCCO1 10.1038/s41467-023-40064-9
CHEMBL306700 102965 35 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 237 5 1 4 1.5 CCOc1ccccc1OCC1CNCCO1 10.1038/s41467-023-40064-9
16362 3103 71 None - 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3103 71 None - 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3103 71 None - 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3103 71 None - 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3103 71 None - 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
4209 3141 75 None -758 34 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 3141 75 None -758 34 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 3141 75 None -758 34 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 3141 75 None -758 34 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 3141 75 None -758 34 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 3141 75 None -758 34 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
319 1312 44 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 1312 44 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 1312 44 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 1312 44 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 1312 44 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 1312 44 None - 9 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
2402 3345 62 None -9 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095 3345 62 None -9 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
7295 3345 62 None -9 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
CHEMBL589 3345 62 None -9 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
DB00268 3345 62 None -9 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
3316 31730 71 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 221 7 1 2 2.7 CCCCCCOc1ccccc1C(N)=O 10.1038/s41467-023-40064-9
CHEMBL1405973 31730 71 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 221 7 1 2 2.7 CCCCCCOc1ccccc1C(N)=O 10.1038/s41467-023-40064-9
216416 111554 48 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111554 48 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
2771 194994 74 None 1 27 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 194994 74 None 1 27 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 194994 74 None 1 27 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
2337 3232 77 None -15 63 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3232 77 None -15 63 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3232 77 None -15 63 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3232 77 None -15 63 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3232 77 None -15 63 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
10007 14452 38 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 2 1 1 2.6 CC(C)(N)Cc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1201269 14452 38 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 183 2 1 1 2.6 CC(C)(N)Cc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
150 2492 21 None 1 16 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1764 2492 21 None 1 16 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226 2492 21 None 1 16 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
CHEMBL1201356 2492 21 None 1 16 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
DB00353 2492 21 None 1 16 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
2771 194994 74 None 1 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 194994 74 None 1 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 194994 74 None 1 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
2099 9275 55 None - 1 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O 10.1038/s41467-023-40064-9
CHEMBL1110 9275 55 None - 1 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O 10.1038/s41467-023-40064-9
1782 2501 84 None -3 23 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
241 2501 84 None -3 23 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
4168 2501 84 None -3 23 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
CHEMBL86 2501 84 None -3 23 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
DB01233 2501 84 None -3 23 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
11626560 200914 94 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 200914 94 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
1427 2000 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2000 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2000 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2000 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2000 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
124087 1377 114 None -5 15 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1377 114 None -5 15 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1377 114 None -5 15 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1377 114 None -5 15 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1377 114 None -5 15 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
1530 2169 50 None -19 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827 2169 50 None -19 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
7206 2169 50 None -19 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
CHEMBL534 2169 50 None -19 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
DB00920 2169 50 None -19 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
55645 84341 8 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
CHEMBL2218861 84341 8 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
11658860 2329 51 None -1 3 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
2941 2329 51 None -1 3 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
4374 2329 51 None -1 3 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
CHEMBL360328 2329 51 None -1 3 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
DB04871 2329 51 None -1 3 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
48041 107054 46 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 6 1 3 4.4 COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1 10.1038/s41467-023-40064-9
CHEMBL315838 107054 46 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 352 6 1 3 4.4 COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1 10.1038/s41467-023-40064-9
1209 1645 75 None -199 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1645 75 None -199 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1645 75 None -199 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1645 75 None -199 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1645 75 None -199 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
134 2497 24 None -2 68 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 2497 24 None -2 68 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 2497 24 None -2 68 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 2497 24 None -2 68 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 2497 24 None -2 68 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1210 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
90475904 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 915 51 None -1380 21 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
11693 1814 16 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494 1814 16 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 1814 16 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 1814 16 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 1814 16 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 1814 16 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
21722 17960 31 None - 6 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17960 31 None - 6 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
242 469 124 None -1 52 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 469 124 None -1 52 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 469 124 None -1 52 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 469 124 None -1 52 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 469 124 None -1 52 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
31101 726 40 None -26 36 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 726 40 None -26 36 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 726 40 None -26 36 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 726 40 None -26 36 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 726 40 None -26 36 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
2162 41484 100 None - 6 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41484 100 None - 6 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
3337 206344 27 None -75 41 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
65801 206344 27 None -75 41 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
66264 206344 27 None -75 41 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
91452 206344 27 None -75 41 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL87493 206344 27 None -75 41 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
3157 1458 71 None -37 12 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 1458 71 None -37 12 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 1458 71 None -37 12 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 1458 71 None -37 12 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 1458 71 None -37 12 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
10531 1408 21 None -15 24 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 1408 21 None -15 24 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 1408 21 None -15 24 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 1408 21 None -15 24 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 1408 21 None -15 24 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
2142 3074 58 None -43 37 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 3074 58 None -43 37 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 3074 58 None -43 37 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 3074 58 None -43 37 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 3074 58 None -43 37 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 3074 58 None -43 37 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4418 34192 85 None - 7 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 34192 85 None - 7 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
150 2492 21 None 1 16 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1764 2492 21 None 1 16 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226 2492 21 None 1 16 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
CHEMBL1201356 2492 21 None 1 16 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
DB00353 2492 21 None 1 16 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
2520 203985 70 None -4 12 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1280 203985 70 None -4 12 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL6966 203985 70 None -4 12 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
123606 351 70 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
128 351 70 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
7110 351 70 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
CHEMBL1505 351 70 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
DB00918 351 70 None - 3 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 10.1038/s41467-023-40064-9
1209 1645 75 None -199 32 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1645 75 None -199 32 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1645 75 None -199 32 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1645 75 None -199 32 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1645 75 None -199 32 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
1212 1649 50 None -27 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 1649 50 None -27 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 1649 50 None -27 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 1649 50 None -27 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 1649 50 None -27 66 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
16231 207486 57 None - 17 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N 10.1038/s41467-023-40064-9
CHEMBL945 207486 57 None - 17 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N 10.1038/s41467-023-40064-9
5360696 1394 30 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
6953 1394 30 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
842 1394 30 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
CHEMBL52440 1394 30 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
DB00514 1394 30 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 271 1 0 2 3.4 COc1ccc2c(c1)[C@@]13CCCC[C@@H]3[C@H](C2)N(CC1)C 10.1038/s41467-023-40064-9
4452 2742 19 None -208 19 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2742 19 None -208 19 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2742 19 None -208 19 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
10531 1408 21 None -15 24 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 1408 21 None -15 24 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 1408 21 None -15 24 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 1408 21 None -15 24 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 1408 21 None -15 24 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
27447 59773 63 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 347 4 3 5 0.4 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1 10.1038/s41467-023-40064-9
6560168 59773 63 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 347 4 3 5 0.4 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1 10.1038/s41467-023-40064-9
CHEMBL1727 59773 63 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 347 4 3 5 0.4 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1 10.1038/s41467-023-40064-9
154257 178595 67 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178595 67 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
2470 3626 50 None -14125 60 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3626 50 None -14125 60 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3626 50 None -14125 60 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3626 50 None -14125 60 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3626 50 None -14125 60 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
2600 3750 74 None -1 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3750 74 None -1 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3750 74 None -1 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3750 74 None -1 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3750 74 None -1 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
1224 1420 83 None -6 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1420 83 None -6 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1420 83 None -6 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1420 83 None -6 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1420 83 None -6 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1420 83 None -6 13 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
2286 3161 51 None -5 30 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3161 51 None -5 30 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3161 51 None -5 30 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3161 51 None -5 30 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3161 51 None -5 30 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
2713 205248 82 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 205248 82 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 205248 82 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 205248 82 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 205248 82 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 205248 82 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 205248 82 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
2389 3306 118 None -66 68 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3306 118 None -66 68 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3306 118 None -66 68 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3306 118 None -66 68 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3306 118 None -66 68 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
3639 168422 106 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 297 1 3 5 -0.4 NS(=O)(=O)c1cc2c(cc1Cl)NCNS2(=O)=O 10.1038/s41467-023-40064-9
CHEMBL435 168422 106 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 297 1 3 5 -0.4 NS(=O)(=O)c1cc2c(cc1Cl)NCNS2(=O)=O 10.1038/s41467-023-40064-9
191 402 98 None -5 29 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 402 98 None -5 29 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 402 98 None -5 29 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 402 98 None -5 29 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 402 98 None -5 29 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
135 2515 43 None -3 58 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2515 43 None -3 58 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2515 43 None -3 58 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2515 43 None -3 58 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2515 43 None -3 58 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2780 110502 36 None - 11 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL325109 110502 36 None - 11 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
72093 35031 9 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35031 9 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35031 9 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
4212 198656 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
CHEMBL1417019 198656 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
CHEMBL58 198656 82 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 444 12 8 10 -0.1 O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21 10.1038/s41467-023-40064-9
4567 9916 34 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL114655 9916 34 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
3062316 33545 121 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL1421 33545 121 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
213 3824 55 None -5 44 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 3824 55 None -5 44 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 3824 55 None -5 44 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 3824 55 None -5 44 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 3824 55 None -5 44 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
135398737 955 93 None -2 92 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 955 93 None -2 92 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 955 93 None -2 92 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 955 93 None -2 92 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 955 93 None -2 92 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
2105 3032 37 None -28 33 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 3032 37 None -28 33 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 3032 37 None -28 33 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 3032 37 None -28 33 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 3032 37 None -28 33 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
37 775 60 None 1 17 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 775 60 None 1 17 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 775 60 None 1 17 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 775 60 None 1 17 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 775 60 None 1 17 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
1234 189197 56 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1256940 189197 56 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL51149 189197 56 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 484 14 0 7 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2cc(OC)c(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
180 400 56 None -35 40 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 400 56 None -35 40 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 400 56 None -35 40 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 400 56 None -35 40 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 400 56 None -35 40 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3152 188387 103 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 188387 103 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
1890 2739 49 None - 16 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2739 49 None - 16 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2739 49 None - 16 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2739 49 None - 16 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2739 49 None - 16 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
214 3831 58 None - 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3831 58 None - 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3831 58 None - 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3831 58 None - 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3831 58 None - 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3831 58 None - 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
212 3777 47 None - 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3777 47 None - 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3777 47 None - 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3777 47 None - 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3777 47 None - 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
102 4096 48 None -93 50 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4096 48 None -93 50 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4096 48 None -93 50 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4096 48 None -93 50 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4096 48 None -93 50 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
198 312 126 None -346 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
82148 312 126 None -346 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
99 312 126 None -346 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
CHEMBL10878 312 126 None -346 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
DB06594 312 126 None -346 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1038/s41467-023-40064-9
8249 59375 65 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 205 3 5 2 0.2 N=C(N)NC(=N)NCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1528839 59375 65 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 205 3 5 2 0.2 N=C(N)NC(=N)NCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL170988 59375 65 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 205 3 5 2 0.2 N=C(N)NC(=N)NCCc1ccccc1 10.1038/s41467-023-40064-9
1222 878 0 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
2678 878 0 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
581 878 0 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1000 878 0 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00341 878 0 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
1016 3720 78 None -17 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 3720 78 None -17 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 3720 78 None -17 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 3720 78 None -17 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 3720 78 None -17 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 3720 78 None -17 35 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
3686 94638 108 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 338 12 1 5 3.5 COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O 10.1038/s41467-023-40064-9
CHEMBL252556 94638 108 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 338 12 1 5 3.5 COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O 10.1038/s41467-023-40064-9
6989 100925 115 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 150 1 1 1 2.8 Cc1ccc(C(C)C)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL29411 100925 115 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 150 1 1 1 2.8 Cc1ccc(C(C)C)c(O)c1 10.1038/s41467-023-40064-9
4886 14078 28 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 293 9 0 4 3.0 CCCCOc1ccc(OCCCN2CCOCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1198 14078 28 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 293 9 0 4 3.0 CCCCOc1ccc(OCCCN2CCOCC2)cc1 10.1038/s41467-023-40064-9
2318 154832 29 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154832 29 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
2726 916 68 None -19 73 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 916 68 None -19 73 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 916 68 None -19 73 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 916 68 None -19 73 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 916 68 None -19 73 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
441074 19382 82 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL1294 19382 82 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR2B in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
10198431 73876 0 None -7 3 Human 9.0 pEC50 = 9.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201930 73876 0 None -7 3 Human 9.0 pEC50 = 9.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
5 139 72 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
5202 139 72 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
CHEMBL39 139 72 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
DB08839 139 72 None -13 55 Human 8.8 pEC50 = 8.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
44407335 73065 0 None -7 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
CHEMBL201117 73065 0 None -7 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
44407440 139281 0 None -4 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL379223 139281 0 None -4 3 Human 6.9 pEC50 = 6.9 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
18715554 74395 0 None -10 3 Human 6.8 pEC50 = 6.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202656 74395 0 None -10 3 Human 6.8 pEC50 = 6.8 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
18715564 73351 0 None -7 3 Human 8.7 pEC50 = 8.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201454 73351 0 None -7 3 Human 8.7 pEC50 = 8.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
18715555 74346 0 None -8 3 Human 7.7 pEC50 = 7.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
CHEMBL202458 74346 0 None -8 3 Human 7.7 pEC50 = 7.7 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
135398737 955 93 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 955 93 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 955 93 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 955 93 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 955 93 None -2 92 Human 7.7 pEC50 = 7.7 Binding
Inverse agonist activity at human 5HT2B receptor by R-SAT assayInverse agonist activity at human 5HT2B receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44407398 74389 0 None -8 3 Human 7.6 pEC50 = 7.6 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
CHEMBL202616 74389 0 None -8 3 Human 7.6 pEC50 = 7.6 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
5 139 72 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
5202 139 72 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
CHEMBL39 139 72 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
DB08839 139 72 None -29 55 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secsAgonist activity at 5HT2b receptor in Wistar rat fundus measured for 90 secs
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2015.08.051
166 3334 18 None 1 3 Human 8.4 pEC50 = 8.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
3045227 3334 18 None 1 3 Human 8.4 pEC50 = 8.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
CHEMBL76781 3334 18 None 1 3 Human 8.4 pEC50 = 8.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
44407453 74374 0 None -9 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
CHEMBL202538 74374 0 None -9 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
18715561 73015 0 None -4 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201062 73015 0 None -4 3 Human 7.4 pEC50 = 7.4 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
44407327 141222 0 None -5 3 Human 6.3 pEC50 = 6.3 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL383042 141222 0 None -5 3 Human 6.3 pEC50 = 6.3 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
18715558 73853 0 None -5 3 Human 7.2 pEC50 = 7.2 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201897 73853 0 None -5 3 Human 7.2 pEC50 = 7.2 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
9901086 187607 33 None - 2 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at 5HT2B receptor (unknown origin) relative to controlAgonist activity at 5HT2B receptor (unknown origin) relative to control
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm5019274
CHEMBL494947 187607 33 None - 2 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at 5HT2B receptor (unknown origin) relative to controlAgonist activity at 5HT2B receptor (unknown origin) relative to control
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm5019274
44407337 74175 0 None -5 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202324 74175 0 None -5 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
44407460 140325 0 None -6 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
CHEMBL380763 140325 0 None -6 3 Human 7.0 pEC50 = 7.0 Binding
Binding to human 5HT2B receptor expressed in CHO cellsBinding to human 5HT2B receptor expressed in CHO cells
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
CHEMBL5081637 214734 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL None None None CN(CCc1cn(C)c2cccc(O)c12)CC1CC1 10.1021/acsmedchemlett.1c00578
133 2479 52 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2479 52 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2479 52 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2479 52 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2479 52 None -2 43 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
134 2497 24 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2497 24 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2497 24 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2497 24 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2497 24 None -2 68 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
11291 3196 26 None - 5 Human 9.0 pIC50 = 9.0 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00578
4980 3196 26 None - 5 Human 9.0 pIC50 = 9.0 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00578
CHEMBL65547 3196 26 None - 5 Human 9.0 pIC50 = 9.0 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00578
150 2492 21 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2492 21 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2492 21 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2492 21 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2492 21 None 1 16 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
191 402 98 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 402 98 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 402 98 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 402 98 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 402 98 None -5 29 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2099 9275 55 None - 1 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL1110 9275 55 None - 1 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
11518143 89037 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 454 12 1 5 4.0 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2Cc2ccccc2)C(C)C)ccc1OC 10.1021/jm3017078
CHEMBL2322611 89037 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 454 12 1 5 4.0 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2Cc2ccccc2)C(C)C)ccc1OC 10.1021/jm3017078
CHEMBL2365004 89037 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 454 12 1 5 4.0 COCCCOc1cc(C(=O)N(C[C@@H]2CNC[C@H]2Cc2ccccc2)C(C)C)ccc1OC 10.1021/jm3017078
2274 3151 58 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3151 58 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3151 58 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3151 58 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3151 58 None -10 32 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
25060119 104288 0 None -9332 7 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
CHEMBL3099899 104288 0 None -9332 7 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
3033538 1307 39 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
7155 1307 39 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
781 1307 39 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
CHEMBL1201216 1307 39 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
DB00298 1307 39 None -12 9 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
213 3824 55 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3824 55 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3824 55 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3824 55 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3824 55 None -5 44 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
12488 1644 56 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1644 56 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1644 56 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1644 56 None -11 23 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
135398737 955 93 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 955 93 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 955 93 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 955 93 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 955 93 None -2 92 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
73453 29585 24 None -9 17 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29585 24 None -9 17 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
25070577 111639 4 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286557 111639 4 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
240 941 43 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 941 43 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 941 43 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 941 43 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 941 43 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 941 43 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 941 43 None -6 25 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
146159245 188426 30 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
451415 188426 30 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
86289437 188426 30 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
CHEMBL502620 188426 30 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
1224 1420 83 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1420 83 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1420 83 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1420 83 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1420 83 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1420 83 None -6 13 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
4178 195780 63 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
CHEMBL558 195780 63 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
44190762 176856 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from 5HT2B receptorDisplacement of radioligand from 5HT2B receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 176856 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from 5HT2B receptorDisplacement of radioligand from 5HT2B receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
222757 99348 73 None -1 3 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
CHEMBL282575 99348 73 None -1 3 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
2812 4747 101 None -40 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4747 101 None -40 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
2247 504 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 504 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 504 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 504 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 504 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
23027035 198524 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
CHEMBL578170 198524 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
78319901 159210 35 None - 0 Human 5.9 pIC50 = 5.9 Binding
Selectivity interaction (Enzymatic assay (PanLabs Profiling)) EUB0000715a HTR2BSelectivity interaction (Enzymatic assay (PanLabs Profiling)) EUB0000715a HTR2B
ChEMBL 379 4 1 6 3.6 C[C@@H]1CN(c2cc(-c3n[nH]c4ccc(OC5(C)CC5)cc34)ncn2)C[C@H](C)O1 10.6019/CHEMBL5212743
CHEMBL4098877 159210 35 None - 0 Human 5.9 pIC50 = 5.9 Binding
Selectivity interaction (Enzymatic assay (PanLabs Profiling)) EUB0000715a HTR2BSelectivity interaction (Enzymatic assay (PanLabs Profiling)) EUB0000715a HTR2B
ChEMBL 379 4 1 6 3.6 C[C@@H]1CN(c2cc(-c3n[nH]c4ccc(OC5(C)CC5)cc34)ncn2)C[C@H](C)O1 10.6019/CHEMBL5212743
54764239 68837 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922537 68837 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
2726 916 68 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 916 68 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 916 68 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 916 68 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 916 68 None -19 73 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
76072441 153923 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 7 0 4 3.4 C=CCN1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
CHEMBL3983539 153923 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 7 0 4 3.4 C=CCN1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
100 3776 58 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3776 58 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3776 58 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3776 58 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3776 58 None -11 56 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
134551 357 27 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 357 27 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 357 27 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 357 27 None -6 21 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
23027211 197227 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568400 197227 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
100951644 169610 16 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 411 7 2 9 2.3 CO[C@H](C(=O)Nc1nnc(N[C@@H]2CCN(c3cccnn3)C2)s1)c1ccccc1 10.1021/acs.jmedchem.9b00260
CHEMBL4437106 169610 16 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 411 7 2 9 2.3 CO[C@H](C(=O)Nc1nnc(N[C@@H]2CCN(c3cccnn3)C2)s1)c1ccccc1 10.1021/acs.jmedchem.9b00260
3042 1402 35 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1402 35 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1402 35 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1402 35 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1402 35 None -39 15 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
5591 157507 90 None 1 2 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
CHEMBL408 157507 90 None 1 2 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
3168 9230 92 None -107 22 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9230 92 None -107 22 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
127048333 140655 1 None 38 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815112 140655 1 None 38 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
1971 2846 38 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2846 38 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2846 38 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2846 38 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2846 38 None -4 30 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
1548953 207656 27 None -4 17 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207656 27 None -4 17 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
5870 31630 92 None - 1 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
CHEMBL1405 31630 92 None - 1 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
6319 23443 95 None - 1 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
CHEMBL1333512 23443 95 None - 1 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
1305 510 14 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 510 14 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 510 14 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
121318543 177543 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 560 6 0 6 4.7 COc1c(S(C)(=O)=O)ccc(O[C@@H](C)C(F)(F)F)c1C(=O)N1CC(c2ncc(C(F)(F)F)cc2Cl)C1 10.1016/j.bmcl.2020.127214
CHEMBL4640428 177543 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5-HT2B (unknown origin)Inhibition of 5-HT2B (unknown origin)
ChEMBL 560 6 0 6 4.7 COc1c(S(C)(=O)=O)ccc(O[C@@H](C)C(F)(F)F)c1C(=O)N1CC(c2ncc(C(F)(F)F)cc2Cl)C1 10.1016/j.bmcl.2020.127214
16665072 98510 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98510 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
155558726 174784 0 None -19 4 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL4562303 174784 0 None -19 4 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
667590 67765 12 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909048 67765 12 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
44112 121264 48 None -11 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 121264 48 None -11 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
17683252 67767 3 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909051 67767 3 None - 1 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
155565189 175541 0 None -6 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
CHEMBL4579120 175541 0 None -6 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
3525815 74117 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2022867 74117 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
2520 203985 70 None -4 12 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 203985 70 None -4 12 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 203985 70 None -4 12 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
23027245 197105 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 197105 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
10660 14384 58 None -29 12 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14384 58 None -29 12 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
2333 142310 97 None 1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
CHEMBL388590 142310 97 None 1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
2771 194994 74 None 1 27 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 194994 74 None 1 27 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 194994 74 None 1 27 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
104903 56314 17 None -4 6 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56314 17 None -4 6 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
2723 154022 108 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
CHEMBL398440 154022 108 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
1379258 67766 13 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909050 67766 13 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
76072442 146363 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 407 5 0 4 4.0 CC(C)(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
CHEMBL3921628 146363 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 407 5 0 4 4.0 CC(C)(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
11277147 106314 0 None 9 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092759 106314 0 None 9 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139188 106314 0 None 9 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
76072471 153513 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 405 6 0 4 3.8 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCC1 nan
CHEMBL3980023 153513 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 405 6 0 4 3.8 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCC1 nan
11452268 81544 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81544 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT2BInhibition of 5HT2B
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
11957541 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
1229 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
147 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
170617 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
CHEMBL6616 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cellsDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.03.006
11957541 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
1229 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
147 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
170617 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
CHEMBL6616 1446 40 None -2 16 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2016.11.014
9881053 120219 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [3H]5-HT from 5-hydroxytryptamine 2B receptorAbility to displace [3H]5-HT from 5-hydroxytryptamine 2B receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35226 120219 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [3H]5-HT from 5-hydroxytryptamine 2B receptorAbility to displace [3H]5-HT from 5-hydroxytryptamine 2B receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
1201549 594 24 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 594 24 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 594 24 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 594 24 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 594 24 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 594 24 None -26 20 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
5510 205829 100 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
CHEMBL83668 205829 100 None - 1 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
44393396 127271 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3cccc(Cl)c3Cl)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL365882 127271 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3cccc(Cl)c3Cl)cc12 10.1016/j.bmcl.2004.05.051
4122 207602 108 None -3 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
CHEMBL9514 207602 108 None -3 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
1353 1898 93 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1898 93 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1898 93 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1898 93 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1898 93 None -295 86 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
1016 3720 78 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3720 78 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3720 78 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3720 78 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3720 78 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3720 78 None -17 35 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL1909069 209053 0 None -1 3 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
1343 1876 62 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1876 62 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1876 62 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1876 62 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1876 62 None -14 9 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
2337 3232 77 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3232 77 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3232 77 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3232 77 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3232 77 None -15 63 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
122196341 124247 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human 5HT2bAntagonist activity at human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
CHEMBL3634745 124247 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human 5HT2bAntagonist activity at human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
2585 800 103 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 800 103 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 800 103 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 800 103 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 800 103 None -18 22 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2389 3306 118 None -66 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3306 118 None -66 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3306 118 None -66 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3306 118 None -66 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3306 118 None -66 68 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
2398 951 62 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 951 62 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 951 62 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 951 62 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 951 62 None -3 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
1605 2327 117 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
3957 2327 117 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
7216 2327 117 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
CHEMBL998 2327 117 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
DB00455 2327 117 None -1 4 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
45482789 198902 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 198902 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
122185011 122538 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 339 3 0 3 5.0 COc1ccc2c([C@H]3CCc4ccc(Cl)cc43)nccc2c1OC 10.1039/C4MD00113C
CHEMBL3601563 122538 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 339 3 0 3 5.0 COc1ccc2c([C@H]3CCc4ccc(Cl)cc43)nccc2c1OC 10.1039/C4MD00113C
11080 29054 79 None -6 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29054 79 None -6 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
3151 1450 97 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1450 97 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1450 97 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1450 97 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1450 97 None -125 27 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
5818 3764 47 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 10.1021/jm401431x
5886965 3764 47 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 10.1021/jm401431x
CHEMBL1368005 3764 47 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 10.1021/jm401431x
76072440 149326 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 393 6 0 4 3.6 CC(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
CHEMBL3945224 149326 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 393 6 0 4 3.6 CC(C)N1CC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)OC1=O nan
1227 2472 43 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 2472 43 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 2472 43 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 2472 43 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 2472 43 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 2472 43 None -112 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
42636941 178925 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL470432 178925 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 5 0 5 4.4 CCCN1CCC(COc2nc3scc(C)c3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
1524 2168 96 None -229 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
197 2168 96 None -229 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
3822 2168 96 None -229 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
88 2168 96 None -229 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
CHEMBL51 2168 96 None -229 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
DB12465 2168 96 None -229 52 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
119584 2577 102 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 2577 102 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 2577 102 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 2577 102 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 2577 102 None 1 6 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
76072443 151554 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 6 0 4 3.4 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CC1 nan
CHEMBL3963333 151554 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 391 6 0 4 3.4 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CC1 nan
11957541 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
1229 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
147 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
170617 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
CHEMBL6616 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.bmc.2013.03.016
11957541 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
1229 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
147 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
170617 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
CHEMBL6616 1446 40 None -2 16 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
72548703 161543 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]+/-DOI from human recombinant 5-HT2B receptor after 60 mins by scintillation counting analysisDisplacement of [125I]+/-DOI from human recombinant 5-HT2B receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161543 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]+/-DOI from human recombinant 5-HT2B receptor after 60 mins by scintillation counting analysisDisplacement of [125I]+/-DOI from human recombinant 5-HT2B receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
1043 1569 14 None -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1569 14 None -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1569 14 None -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1569 14 None -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1569 14 None -22 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
23027527 196769 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 196769 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
23027411 198497 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577912 198497 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
5318 15544 49 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15544 49 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15544 49 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
1531 2253 69 None -16 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2253 69 None -16 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2253 69 None -16 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2253 69 None -16 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2253 69 None -16 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
124 2960 47 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2960 47 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2960 47 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2960 47 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2960 47 None -181 33 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
45485062 197145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 197145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
44404883 72033 32 None -2 4 Human 7.5 pIC50 = 7.5 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
CHEMBL197664 72033 32 None -2 4 Human 7.5 pIC50 = 7.5 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
15987265 196864 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL566075 196864 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
3191 102831 97 None -7 25 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102831 97 None -7 25 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
448537 160226 89 None -21 25 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160226 89 None -21 25 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
5897 105184 80 None -1 3 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
CHEMBL311469 105184 80 None -1 3 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
72197486 102476 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 102476 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 102476 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
45484995 198496 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 198496 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]rauwolsine from human 5HT2B receptorDisplacement of [3H]rauwolsine from human 5HT2B receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
127048335 140567 1 None 15 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813726 140567 1 None 15 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
196129 67769 17 None -26 15 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67769 17 None -26 15 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
4011 82379 49 None -20 24 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82379 49 None -20 24 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
4601 206724 35 None -4 17 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206724 35 None -4 17 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206724 35 None -4 17 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
68617 205504 62 None -15 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 205504 62 None -15 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 205504 62 None -15 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
165193 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3165 68 None -72 43 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2353 101085 82 None -7 5 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 101085 82 None -7 5 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 101085 82 None -7 5 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
3117 207818 103 None -8 16 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207818 103 None -8 16 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
2284 3160 33 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3160 33 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3160 33 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3160 33 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3160 33 None -16 29 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
11304816 66249 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL184717 66249 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
11536844 115096 0 None 1 2 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343672 115096 0 None 1 2 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
2351 3261 64 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3261 64 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3261 64 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3261 64 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3261 64 None -7 21 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
444795 139974 105 None 3 2 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
CHEMBL38 139974 105 None 3 2 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
26987 946 33 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 946 33 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 946 33 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 946 33 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 946 33 None -47 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
72734860 103930 0 None 6 5 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092753 103930 0 None 6 5 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysisAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
3973 208157 110 None -44 3 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
CHEMBL98350 208157 110 None -44 3 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
3157 1458 71 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1458 71 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1458 71 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1458 71 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1458 71 None -37 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
58438464 3043 35 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 3043 35 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 3043 35 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 3043 35 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
6726 1269 51 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1269 51 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1269 51 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1269 51 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1269 51 None -7 13 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
118112300 155970 18 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5HT2B (unknown origin)Antagonist activity at 5HT2B (unknown origin)
ChEMBL 430 6 2 6 3.8 O=S(=O)(Nc1nccs1)c1cc(Cl)c(NCC23CCCN2CCC3)cc1F 10.1016/j.bmcl.2017.03.085
CHEMBL4061793 155970 18 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5HT2B (unknown origin)Antagonist activity at 5HT2B (unknown origin)
ChEMBL 430 6 2 6 3.8 O=S(=O)(Nc1nccs1)c1cc(Cl)c(NCC23CCCN2CCC3)cc1F 10.1016/j.bmcl.2017.03.085
2142 3074 58 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3074 58 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3074 58 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3074 58 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3074 58 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3074 58 None -43 37 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
1212 1649 50 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1649 50 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1649 50 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1649 50 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1649 50 None -27 66 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
11957541 1446 40 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
1229 1446 40 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
147 1446 40 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
170617 1446 40 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
CHEMBL6616 1446 40 None -2 16 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
1042 1568 23 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1568 23 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1568 23 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1568 23 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1568 23 None -7 17 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
44393215 66633 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 417 6 2 4 5.4 Cc1cc(NC(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL185376 66633 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 417 6 2 4 5.4 Cc1cc(NC(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
78243717 137325 53 None - 0 Human 5.4 pIC50 = 5.4 Binding
Selectivity interaction (CEREP panel (cellular receptors and 30 other enzymes)) EUB0000199c HTR2BSelectivity interaction (CEREP panel (cellular receptors and 30 other enzymes)) EUB0000199c HTR2B
ChEMBL 321 4 1 5 2.4 O=C(/C=C/N1C[C@H]2C[C@@H]1CN2c1ccccn1)c1ccccc1O 10.6019/CHEMBL5212743
CHEMBL3752911 137325 53 None - 0 Human 5.4 pIC50 = 5.4 Binding
Selectivity interaction (CEREP panel (cellular receptors and 30 other enzymes)) EUB0000199c HTR2BSelectivity interaction (CEREP panel (cellular receptors and 30 other enzymes)) EUB0000199c HTR2B
ChEMBL 321 4 1 5 2.4 O=C(/C=C/N1C[C@H]2C[C@@H]1CN2c1ccccn1)c1ccccc1O 10.6019/CHEMBL5212743
74538762 143516 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 419 6 0 4 4.2 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCCC1 nan
CHEMBL3898995 143516 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.Radiolabel Binding Assay: A solution of the compound of the disclosure to be tested is prepared as a 1-mg/ml stock in Assay Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) or DMSO according to its solubility. A 1-mg/ml stock of the reference compound 5-hydroxytryptamine (5-HT) is also prepared as a positive control. Eleven dilutions (5x assay concentration) of the compound of the disclosure and 5-HT are prepared in the Assay Buffer by serial dilution to yield final corresponding assay concentrations ranging from 10 uM to 10 uM.A stock concentration of 5 nM [3H]LSD (lysergic acid diethyl amide) is prepared in Assay Buffer. Aliquots (50 ul) of radioligand are dispensed into the wells of a 96-well plate containing 100 ul of Assay Buffer. Duplicate 50-ul aliquots of the compound of the disclosure test and 5-HT positive control reference compound serial dilutions are added. Membrane fractions of cells expressing recombinant 5HT2B receptors (50 uL) are dispensed into each well. The membranes are prepared from stably transfected c ell lines expressing 5HT2B receptors cultured on 10-cm plates by harvesting PBS-rinsed monolayers, resuspending and lysing the monolayers in chilled, hypotonic 50 mM Tris-HCl, pH 7.4, centrifuging at 20,000xg, decanting the supernatant and storing at -80° C. The membrane preparations are resuspended in 3 ml of chilled Assay Buffer and homogenized by several passages through a 26 gauge needle before use in the assay.
ChEMBL 419 6 0 4 4.2 O=C1OC(CN2CCN(C(c3ccccc3)c3ccccc3)CC2)CN1C1CCCC1 nan
1599 2326 50 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2326 50 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2326 50 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2326 50 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2326 50 None -144 16 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
165193 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3165 68 None -72 43 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4209 3141 75 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3141 75 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3141 75 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3141 75 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3141 75 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3141 75 None -758 34 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL5079070 214581 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL None None None CC(C)N(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
124087 1377 114 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1377 114 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1377 114 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1377 114 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1377 114 None -5 15 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
72198754 90851 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392349 90851 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
58438475 92244 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
CHEMBL2426677 92244 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
21138 98423 39 None -6 7 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 98423 39 None -6 7 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
10389430 125925 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL364863 125925 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human 5-HT2B receptorInhibitory activity against human 5-HT2B receptor
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
1530 2169 50 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2169 50 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2169 50 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2169 50 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2169 50 None -19 21 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
5353853 17954 47 None -23 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17954 47 None -23 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17954 47 None -23 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2600 3750 74 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3750 74 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3750 74 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3750 74 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3750 74 None -1 13 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
4211 57792 83 None -2 4 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57792 83 None -2 4 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
6761 67770 19 None -7 18 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67770 19 None -7 18 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
1588 2311 27 None -6 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2311 27 None -6 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2311 27 None -6 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2311 27 None -6 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2311 27 None -6 44 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
206 2476 16 None -1 25 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
68848 2476 16 None -1 25 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL12314 2476 16 None -1 25 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
44516817 57633 5 None -4365 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57633 5 None -4365 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT2B receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
6075 150084 42 None -8 16 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150084 42 None -8 16 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
5624 32663 14 None 5 10 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32663 14 None 5 10 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32663 14 None 5 10 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
11694810 120513 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation countingInhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310123 120513 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation countingInhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545474 120513 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation countingInhibition of human 5-HT2B receptor expressed in HEK293-EBNA cells assessed as [3H]PI metabolism by by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
44592109 179063 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL471663 179063 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 343 6 0 5 4.4 CCCCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
56645363 121464 12 None -2 4 Human 5.3 pIC50 = 5.3 Binding
Selectivity interaction (Enzyme panel (Eurofins-Panlabs radioligand binding assays)) EUB0000313b HTR2BSelectivity interaction (Enzyme panel (Eurofins-Panlabs radioligand binding assays)) EUB0000313b HTR2B
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 10.6019/CHEMBL5212743
CHEMBL3582478 121464 12 None -2 4 Human 5.3 pIC50 = 5.3 Binding
Selectivity interaction (Enzyme panel (Eurofins-Panlabs radioligand binding assays)) EUB0000313b HTR2BSelectivity interaction (Enzyme panel (Eurofins-Panlabs radioligand binding assays)) EUB0000313b HTR2B
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 10.6019/CHEMBL5212743
169713 80132 20 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
CHEMBL21343 80132 20 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
4943 193393 105 None 1 2 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
CHEMBL526 193393 105 None 1 2 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
11500509 120555 0 None -3 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343670 120555 0 None -3 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545812 120555 0 None -3 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
4189 206899 96 None -26 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206899 96 None -26 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206899 96 None -26 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
2683 102861 25 None -501 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102861 25 None -501 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102861 25 None -501 16 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
3598 187797 76 None -2 7 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 187797 76 None -2 7 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
135398745 2893 112 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2893 112 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2893 112 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2893 112 None -5 66 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
107715 200922 22 None -14 20 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 200922 22 None -14 20 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 200922 22 None -14 20 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
122196341 124247 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human 5HT2bBinding affinity to human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
CHEMBL3634745 124247 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human 5HT2bBinding affinity to human 5HT2b
ChEMBL 422 5 1 3 6.0 O=c1ccc(-c2ccc(OCc3ccc4ccccc4n3)cc2)c(-c2ccc(F)cc2)[nH]1 10.1021/acs.jmedchem.5b01240
10531 1408 21 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1408 21 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1408 21 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1408 21 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1408 21 None -15 24 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
1836 2574 59 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2574 59 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2574 59 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2574 59 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2574 59 None -69 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
14049689 198420 11 None 20 2 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
CHEMBL577294 198420 11 None 20 2 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
72198756 90853 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 478 8 0 5 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3c(Cl)nc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392351 90853 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 478 8 0 5 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3c(Cl)nc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
1782 2501 84 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
241 2501 84 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
4168 2501 84 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
CHEMBL86 2501 84 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
DB01233 2501 84 None -3 23 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
72713752 103716 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 396 5 2 7 3.0 Cc1csc(C(C)(O)c2nnc(NC(=O)Cc3c(F)cccc3F)s2)n1 10.1021/jm4012033
CHEMBL3088176 103716 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 396 5 2 7 3.0 Cc1csc(C(C)(O)c2nnc(NC(=O)Cc3c(F)cccc3F)s2)n1 10.1021/jm4012033
90644511 111638 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
CHEMBL3286556 111638 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
2406 100376 89 None -27 12 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 100376 89 None -27 12 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
2286 3161 51 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3161 51 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3161 51 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3161 51 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3161 51 None -5 30 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
3198 205490 76 None -30 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205490 76 None -30 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205490 76 None -30 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
135 2515 43 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2515 43 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2515 43 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2515 43 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2515 43 None -3 58 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
180 400 56 None -35 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 400 56 None -35 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 400 56 None -35 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 400 56 None -35 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 400 56 None -35 40 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
4595 176691 106 None 2 15 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL46 176691 106 None 2 15 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
11536843 115097 0 None 1 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343673 115097 0 None 1 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolismAntagonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as [3H]PI metabolism
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
1547484 937 74 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 937 74 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 937 74 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 937 74 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 937 74 None -8 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
102 4096 48 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4096 48 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4096 48 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4096 48 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4096 48 None -93 50 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
2477 742 59 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
36 742 59 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
437 742 59 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
CHEMBL49 742 59 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
DB00490 742 59 None -13 29 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
71499384 111122 41 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 448 8 1 5 4.5 COc1cc(/C=C/C(=O)NCCn2c(C(F)(F)F)cc3ccccc32)cc(OC)c1OC 10.1021/jm401431x
CHEMBL3264204 111122 41 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 448 8 1 5 4.5 COc1cc(/C=C/C(=O)NCCn2c(C(F)(F)F)cc3ccccc32)cc(OC)c1OC 10.1021/jm401431x
2105 3032 37 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3032 37 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3032 37 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3032 37 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3032 37 None -28 33 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
67406727 117166 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394201 117166 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
11957735 199998 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 350 4 1 5 4.0 CN(C)Cc1nc(-c2ccc(C(C)(C)C)cc2)n(-c2cccc(O)c2)n1 10.1016/j.bmc.2009.07.007
CHEMBL595449 199998 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 350 4 1 5 4.0 CN(C)Cc1nc(-c2ccc(C(C)(C)C)cc2)n(-c2cccc(O)c2)n1 10.1016/j.bmc.2009.07.007
2028 2958 80 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2958 80 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2958 80 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2958 80 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2958 80 None -40 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
31101 726 40 None -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 726 40 None -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 726 40 None -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 726 40 None -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 726 40 None -26 36 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
161 751 6 None 2 6 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 751 6 None 2 6 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 751 6 None 2 6 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
54764240 68839 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922539 68839 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL5085055 214923 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assayModulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay
ChEMBL None None None CCN(C)CCc1cn(C)c2cccc(O)c12 10.1021/acsmedchemlett.1c00578
4098 32475 30 None -14 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32475 30 None -14 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32475 30 None -14 11 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
54764241 68838 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922538 68838 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
5282379 194961 69 None 1 3 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
CHEMBL547 194961 69 None 1 3 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
146420029 184738 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 379 3 1 3 4.2 CN1CCC(=C(F)c2cccc(NC(=O)c3c(F)cc(F)cc3F)n2)CC1 10.1016/j.ejmech.2021.113782
CHEMBL4851044 184738 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 379 3 1 3 4.2 CN1CCC(=C(F)c2cccc(NC(=O)c3c(F)cc(F)cc3F)n2)CC1 10.1016/j.ejmech.2021.113782
3158 56237 27 None -389 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56237 27 None -389 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
72197484 102467 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 102467 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 102467 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-lysergic acid from human recombinant 5HT-2B receptorDisplacement of [3H]-lysergic acid from human recombinant 5HT-2B receptor
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
277 1289 62 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1289 62 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1289 62 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1289 62 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1289 62 None -5 46 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
1305 510 14 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]LSD from human 5HT2B receptorDisplacement of [125I]LSD from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 510 14 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]LSD from human 5HT2B receptorDisplacement of [125I]LSD from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 510 14 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]LSD from human 5HT2B receptorDisplacement of [125I]LSD from human 5HT2B receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9861687 189175 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 315 4 0 5 3.7 CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
CHEMBL511312 189175 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptorDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor
ChEMBL 315 4 0 5 3.7 CCN1CCC(COc2nc3ccsc3n3cccc23)CC1 10.1016/j.bmc.2008.11.045
2291 3162 58 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3162 58 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3162 58 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3162 58 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3162 58 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
176 397 66 None -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 397 66 None -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 397 66 None -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 397 66 None -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 397 66 None -1 31 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
657255 199061 34 None -9 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199061 34 None -9 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
3952 1875 38 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1875 38 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1875 38 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1875 38 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1875 38 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1875 38 None -3 12 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
24360 203321 106 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
CHEMBL65 203321 106 None - 1 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
127048334 140575 1 None 13 3 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813796 140575 1 None 13 3 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human 5-HT2B receptor by PDSP assayAntagonist activity at human 5-HT2B receptor by PDSP assay
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
10851262 40529 0 None 1 2 Rat 8.9 pKd = 8.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 293 1 1 3 3.7 Cc1coc2cc3c(cc12)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL148346 40529 0 None 1 2 Rat 8.9 pKd = 8.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 293 1 1 3 3.7 Cc1coc2cc3c(cc12)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
9972439 40581 0 None -1 2 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 2 1 3 3.7 CCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL148385 40581 0 None -1 2 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 2 1 3 3.7 CCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
10851406 119238 1 None -1 2 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 295 1 1 3 3.9 O=C(Nc1cccnc1)N1CCc2cc3sccc3cc21 10.1021/jm960571v
CHEMBL343666 119238 1 None -1 2 Rat 8.0 pKd = 8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 295 1 1 3 3.9 O=C(Nc1cccnc1)N1CCc2cc3sccc3cc21 10.1021/jm960571v
141 1415 35 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
6089 1415 35 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
CHEMBL12420 1415 35 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
DB01488 1415 35 None -11 22 Rat 6.0 pKd = 6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm00343a013
12281266 31802 5 None - 1 Rat 7.0 pKd = 7.0 Binding
Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.
ChEMBL 187 3 0 1 3.7 CC(C)CCn1ccc2ccccc21 10.1021/jm00367a008
CHEMBL140663 31802 5 None - 1 Rat 7.0 pKd = 7.0 Binding
Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.Compound was tested for serotonin receptor affinity by the displacement of [3H]- -5-HT binding to rat fundus membranes.
ChEMBL 187 3 0 1 3.7 CC(C)CCn1ccc2ccccc21 10.1021/jm00367a008
6088 119816 56 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 10.1021/jm00343a013
CHEMBL348588 119816 56 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 10.1021/jm00343a013
10637557 36241 0 None 5 2 Rat 7.9 pKd = 7.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 294 1 1 3 2.7 CN1CCc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL144567 36241 0 None 5 2 Rat 7.9 pKd = 7.9 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 294 1 1 3 2.7 CN1CCc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
152234 55993 22 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1cccc(CC(C)N)c1 10.1021/jm00144a009
CHEMBL16247 55993 22 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1cccc(CC(C)N)c1 10.1021/jm00144a009
44359526 116605 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2c(ccn2CCC(C)C)c1 10.1021/jm00367a008
CHEMBL336928 116605 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2c(ccn2CCC(C)C)c1 10.1021/jm00367a008
44359525 28840 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
CHEMBL137933 28840 1 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
805647 30780 12 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 189 3 0 3 1.6 CN(C)CCn1cnc2ccccc21 10.1021/jm00367a008
CHEMBL139655 30780 12 None - 1 Rat 6.9 pKd = 6.9 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 189 3 0 3 1.6 CN(C)CCn1cnc2ccccc21 10.1021/jm00367a008
143435 99666 6 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(CC(C)N)cc1OC 10.1021/jm00144a009
CHEMBL284589 99666 6 None - 1 Rat 5.9 pKd = 5.9 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(CC(C)N)cc1OC 10.1021/jm00144a009
62787 206165 21 None -3 10 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 10.1021/jm00144a009
CHEMBL8642 206165 21 None -3 10 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 10.1021/jm00144a009
9904139 106966 1 None 1 4 Rat 7.8 pKd = 7.8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm960571v
CHEMBL315223 106966 1 None 1 4 Rat 7.8 pKd = 7.8 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm960571v
31014 205868 20 None 2 3 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(OC)cc1CC(C)N 10.1021/jm00144a009
CHEMBL8389 205868 20 None 2 3 Rat 6.8 pKd = 6.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(OC)cc1CC(C)N 10.1021/jm00144a009
144891 107360 8 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 241 5 1 4 2.3 COc1cc(OC)c(SC)cc1CC(C)N 10.1021/jm00144a009
CHEMBL31787 107360 8 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 241 5 1 4 2.3 COc1cc(OC)c(SC)cc1CC(C)N 10.1021/jm00144a009
9904139 106966 1 None 1 4 Rat 7.8 pKd = 7.8 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm00014a004
CHEMBL315223 106966 1 None 1 4 Rat 7.8 pKd = 7.8 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CC3 10.1021/jm00014a004
141685 107021 6 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(CC(C)N)cc1OC 10.1021/jm00144a009
CHEMBL31557 107021 6 None - 1 Rat 5.8 pKd = 5.8 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(CC(C)N)cc1OC 10.1021/jm00144a009
11806221 120196 1 None - 1 Rat 6.7 pKd = 6.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)C(CCN(C)C)CN2 10.1021/jm00343a013
CHEMBL352140 120196 1 None - 1 Rat 6.7 pKd = 6.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)C(CCN(C)C)CN2 10.1021/jm00343a013
10757038 119208 0 None 1 2 Rat 7.7 pKd = 7.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 1 1 3 3.5 Cc1cc2cc3c(cc2n1C)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL343455 119208 0 None 1 2 Rat 7.7 pKd = 7.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 306 1 1 3 3.5 Cc1cc2cc3c(cc2n1C)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
10690384 120930 0 None -3 2 Rat 6.7 pKd = 6.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 368 3 1 3 4.7 O=C(Nc1cccnc1)N1CCc2cc3c(ccn3Cc3ccccc3)cc21 10.1021/jm960571v
CHEMBL356146 120930 0 None -3 2 Rat 6.7 pKd = 6.7 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 368 3 1 3 4.7 O=C(Nc1cccnc1)N1CCc2cc3c(ccn3Cc3ccccc3)cc21 10.1021/jm960571v
44359444 29098 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
CHEMBL138144 29098 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 217 4 0 2 3.7 COc1ccc2ccn(CCC(C)C)c2c1 10.1021/jm00367a008
12655251 119283 58 None - 1 Rat 5.7 pKd = 5.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 162 2 2 2 1.5 NCCC1CNc2ccccc21 10.1021/jm00367a008
CHEMBL344028 119283 58 None - 1 Rat 5.7 pKd = 5.7 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 162 2 2 2 1.5 NCCC1CNc2ccccc21 10.1021/jm00367a008
11074217 52777 4 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 190 3 1 2 2.1 CN(C)CCC1CNc2ccccc21 10.1021/jm00343a013
CHEMBL159503 52777 4 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 190 3 1 2 2.1 CN(C)CCC1CNc2ccccc21 10.1021/jm00343a013
547452 54761 2 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 187 3 0 1 2.6 CN(C)CCC1=CCc2ccccc21 10.1021/jm00343a013
CHEMBL161241 54761 2 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 187 3 0 1 2.6 CN(C)CCC1=CCc2ccccc21 10.1021/jm00343a013
12451869 55154 5 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL161751 55154 5 None - 1 Rat 5.7 pKd = 5.7 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
144889 99296 6 None - 1 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(OC)c(CC(C)N)cc1C 10.1021/jm00144a009
CHEMBL282183 99296 6 None - 1 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(OC)c(CC(C)N)cc1C 10.1021/jm00144a009
34677 102192 88 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 147 0 1 1 1.5 NC1CCc2ccccc2C1 10.1021/jm00343a013
CHEMBL30294 102192 88 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 147 0 1 1 1.5 NC1CCc2ccccc2C1 10.1021/jm00343a013
141047 99378 20 None 1 3 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)c(OC)c1 10.1021/jm00144a009
CHEMBL282734 99378 20 None 1 3 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)c(OC)c1 10.1021/jm00144a009
31016 102260 15 None -11 5 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC 10.1021/jm00144a009
CHEMBL30336 102260 15 None -11 5 Rat 5.6 pKd = 5.6 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC 10.1021/jm00144a009
15011362 52616 24 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 161 2 1 1 2.1 NCCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL159346 52616 24 None - 1 Rat 5.6 pKd = 5.6 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 161 2 1 1 2.1 NCCC1CCc2ccccc21 10.1021/jm00343a013
744368 164905 18 None - 1 Rat 6.6 pKd = 6.6 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 190 3 0 2 1.6 CN(C)CCN1CCc2ccccc21 10.1021/jm00367a008
CHEMBL422471 164905 18 None - 1 Rat 6.6 pKd = 6.6 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 190 3 0 2 1.6 CN(C)CCN1CCc2ccccc21 10.1021/jm00367a008
159755 57065 61 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccccc1CC(C)N 10.1021/jm00144a009
CHEMBL16451 57065 61 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccccc1CC(C)N 10.1021/jm00144a009
91255 99083 11 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(CC(C)N)c1OC 10.1021/jm00144a009
CHEMBL280855 99083 11 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(CC(C)N)c1OC 10.1021/jm00144a009
189 3466 39 None 2 17 Rat 8.5 pKd = 8.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm960571v
5163 3466 39 None 2 17 Rat 8.5 pKd = 8.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm960571v
CHEMBL297784 3466 39 None 2 17 Rat 8.5 pKd = 8.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm960571v
189 3466 39 None 2 17 Rat 8.5 pKd = 8.5 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
5163 3466 39 None 2 17 Rat 8.5 pKd = 8.5 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
CHEMBL297784 3466 39 None 2 17 Rat 8.5 pKd = 8.5 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm00014a004
10683987 121252 1 None 3 2 Rat 7.5 pKd = 7.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 278 1 2 2 3.2 O=C(Nc1cccnc1)N1CCc2cc3[nH]ccc3cc21 10.1021/jm960571v
CHEMBL357870 121252 1 None 3 2 Rat 7.5 pKd = 7.5 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 278 1 2 2 3.2 O=C(Nc1cccnc1)N1CCc2cc3[nH]ccc3cc21 10.1021/jm960571v
1614 203632 24 None -2 10 Rat 6.5 pKd = 6.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 10.1021/jm00144a009
CHEMBL6731 203632 24 None -2 10 Rat 6.5 pKd = 6.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 10.1021/jm00144a009
8423 98661 30 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)cc1OC 10.1021/jm00144a009
CHEMBL277540 98661 30 None - 1 Rat 5.5 pKd = 5.5 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1ccc(CC(C)N)cc1OC 10.1021/jm00144a009
126769 206019 42 None -1 5 Rat 7.4 pKd = 7.4 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00014a004
CHEMBL536255 206019 42 None -1 5 Rat 7.4 pKd = 7.4 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00014a004
CHEMBL85194 206019 42 None -1 5 Rat 7.4 pKd = 7.4 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1021/jm00014a004
12451869 55154 5 None - 1 Rat 5.4 pKd = 5.4 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL161751 55154 5 None - 1 Rat 5.4 pKd = 5.4 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 175 3 1 1 2.3 CNCCC1CCc2ccccc21 10.1021/jm00343a013
155 725 25 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
163 725 25 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
62065 725 25 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
CHEMBL6607 725 25 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
DB01484 725 25 None -10 13 Rat 7.4 pKd = 7.4 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 10.1021/jm00144a009
44375004 52976 1 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 189 3 0 1 2.7 CN(C)CCC1CCc2ccccc21 10.1021/jm00343a013
CHEMBL159689 52976 1 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 189 3 0 1 2.7 CN(C)CCC1CCc2ccccc21 10.1021/jm00343a013
44359477 116408 0 None - 1 Rat 7.3 pKd = 7.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2ccn(CCC(C)C)c12 10.1021/jm00367a008
CHEMBL336042 116408 0 None - 1 Rat 7.3 pKd = 7.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2ccn(CCC(C)C)c12 10.1021/jm00367a008
77042 188333 58 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 177 4 0 2 1.8 CN(C)CCC(=O)c1ccccc1 10.1021/jm00343a013
CHEMBL50115 188333 58 None - 1 Rat 5.3 pKd = 5.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 177 4 0 2 1.8 CN(C)CCC(=O)c1ccccc1 10.1021/jm00343a013
31015 118389 16 None - 1 Rat 6.3 pKd = 6.3 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(CC(C)N)c(OC)c1 10.1021/jm00144a009
CHEMBL34108 118389 16 None - 1 Rat 6.3 pKd = 6.3 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1cc(OC)c(CC(C)N)c(OC)c1 10.1021/jm00144a009
10335310 205980 0 None 75 2 Rat 7.3 pKd = 7.3 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2cc3c(cc21)CCCN3C(=O)Nc1cccnc1 10.1021/jm00014a004
CHEMBL84888 205980 0 None 75 2 Rat 7.3 pKd = 7.3 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2cc3c(cc21)CCCN3C(=O)Nc1cccnc1 10.1021/jm00014a004
33984 29610 40 None - 1 Rat 6.3 pKd = 6.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 192 5 0 2 2.1 CCN(CCN(C)C)c1ccccc1 10.1021/jm00367a008
CHEMBL138604 29610 40 None - 1 Rat 6.3 pKd = 6.3 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 192 5 0 2 2.1 CCN(CCN(C)C)c1ccccc1 10.1021/jm00367a008
1150 3849 121 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
125 3849 121 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
CHEMBL6640 3849 121 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
DB08653 3849 121 None -8 25 Rat 6.3 pKd = 6.3 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00343a013
3007 155661 27 None -1 6 Rat 5.3 pKd = 5.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
ChEMBL 135 2 1 1 1.6 CC(N)Cc1ccccc1 10.1021/jm00144a009
CHEMBL405 155661 27 None -1 6 Rat 5.3 pKd = 5.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
ChEMBL 135 2 1 1 1.6 CC(N)Cc1ccccc1 10.1021/jm00144a009
127035062 136426 0 None -4 19 Human 6.3 pKd = 6.3 Binding
Non-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot methodNon-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 136426 0 None -4 19 Human 6.3 pKd = 6.3 Binding
Non-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot methodNon-competitive antagonist activity at human recombinant 5-HT2B receptor stably expressed in HEK cell membrane by schild plot method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
10591799 39920 0 None 1 2 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 2 1 3 4.2 CC(C)n1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL147820 39920 0 None 1 2 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 2 1 3 4.2 CC(C)n1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
44363813 40530 0 None 19 2 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 305 1 1 2 4.1 Cc1cn(C)c2cc3c(cc12)N(C(=O)Nc1ccccc1)CC3 10.1021/jm960571v
CHEMBL148347 40530 0 None 19 2 Rat 8.2 pKd = 8.2 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 305 1 1 2 4.1 Cc1cn(C)c2cc3c(cc12)N(C(=O)Nc1ccccc1)CC3 10.1021/jm960571v
10335309 206023 0 None - 1 Rat 7.2 pKd = 7.2 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CCC3 10.1021/jm00014a004
CHEMBL85247 206023 0 None - 1 Rat 7.2 pKd = 7.2 Binding
Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptorInhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor
ChEMBL 306 1 1 3 3.6 Cn1ccc2c3c(ccc21)N(C(=O)Nc1cccnc1)CCC3 10.1021/jm00014a004
31721 98794 42 None - 1 Rat 5.2 pKd = 5.2 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccc(CC(C)N)cc1 10.1021/jm00144a009
CHEMBL278663 98794 42 None - 1 Rat 5.2 pKd = 5.2 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 165 3 1 2 1.6 COc1ccc(CC(C)N)cc1 10.1021/jm00144a009
10495940 78829 0 None 1 2 Rat 8.1 pKd = 8.1 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 3 1 3 4.0 CCCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
CHEMBL2112859 78829 0 None 1 2 Rat 8.1 pKd = 8.1 Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundusInhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
ChEMBL 320 3 1 3 4.0 CCCn1ccc2cc3c(cc21)CCN3C(=O)Nc1cccnc1 10.1021/jm960571v
44359524 28838 1 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2c1ccn2CCC(C)C 10.1021/jm00367a008
CHEMBL137932 28838 1 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 201 3 0 1 4.0 Cc1cccc2c1ccn2CCC(C)C 10.1021/jm00367a008
164 1448 19 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
85875 1448 19 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
CHEMBL8600 1448 19 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
DB01528 1448 19 None -3 10 Rat 7.1 pKd = 7.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00144a009
141048 102842 9 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(OC)c1CC(C)N 10.1021/jm00144a009
CHEMBL30577 102842 9 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 195 4 1 3 1.6 COc1cccc(OC)c1CC(C)N 10.1021/jm00144a009
25187 100271 28 None - 1 Rat 5.1 pKd = 5.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 163 4 0 1 2.2 CN(C)CCCc1ccccc1 10.1021/jm00343a013
CHEMBL289199 100271 28 None - 1 Rat 5.1 pKd = 5.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 163 4 0 1 2.2 CN(C)CCCc1ccccc1 10.1021/jm00343a013
44359556 119402 0 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)NCC2CCN(C)C 10.1021/jm00367a008
CHEMBL344878 119402 0 None - 1 Rat 7.1 pKd = 7.1 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 220 4 1 3 2.2 COc1ccc2c(c1)NCC2CCN(C)C 10.1021/jm00367a008
145 140 49 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
1832 140 49 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
CHEMBL7257 140 49 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
DB14010 140 49 None -16 30 Rat 7.1 pKd = 7.1 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00343a013
31012 103091 17 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1ccc(CC(C)N)c(OC)c1OC 10.1021/jm00144a009
CHEMBL30777 103091 17 None - 1 Rat 5.1 pKd = 5.1 Binding
Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundusAffinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus
ChEMBL 225 5 1 4 1.6 COc1ccc(CC(C)N)c(OC)c1OC 10.1021/jm00144a009
81206 29619 37 None - 1 Rat 6.0 pKd = 6.0 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00367a008
CHEMBL138614 29619 37 None - 1 Rat 6.0 pKd = 6.0 Binding
Displacement of [3H]5-HT binding to serotonin receptor of rat fundus membranesDisplacement of [3H]5-HT binding to serotonin receptor of rat fundus membranes
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00367a008
81206 29619 37 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00343a013
CHEMBL138614 29619 37 None - 1 Rat 6.0 pKd = 6.0 Binding
The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundusThe binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus
ChEMBL 164 4 1 2 1.7 CN(C)CCNc1ccccc1 10.1021/jm00343a013
CHEMBL5270056 193593 0 None 100 2 Rat 10.1 pKi = 10.1 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 428 4 2 3 5.0 COc1ccc(CC2NCCc3c2[nH]c2c(C)c(C)ccc32)c(Br)c1OC 10.1021/acs.jmedchem.0c01887
CHEMBL5277645 193917 0 None - 1 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 368 5 2 4 4.3 COc1ccc(CC2NCCc3c2[nH]c2cccc(SC)c32)cc1OC 10.1021/acs.jmedchem.0c01887
CHEMBL5279881 194018 0 None - 1 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 350 5 2 3 4.2 CCc1cccc2[nH]c3c(c12)CCNC3Cc1ccc(OC)c(OC)c1 10.1021/acs.jmedchem.0c01887
CHEMBL5280131 194029 0 None - 1 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 448 4 2 3 4.2 COc1ccc(CC2NCCc3c2[nH]c2cccc(I)c32)cc1OC 10.1021/acs.jmedchem.0c01887
CHEMBL5284094 194220 0 None - 1 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 336 4 2 3 3.9 COc1ccc(CC2NCCc3c2[nH]c2cccc(C)c32)cc1OC 10.1021/acs.jmedchem.0c01887
11666595 120506 0 None 301 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1c(Cl)cccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310115 120506 0 None 301 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1c(Cl)cccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545467 120506 0 None 301 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1c(Cl)cccc1-2 10.1016/j.bmc.2014.05.027
9839057 41364 4 None -9 3 Human 9.7 pKi = 9.7 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 293 2 1 3 3.8 CC(N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm9803525
CHEMBL149024 41364 4 None -9 3 Human 9.7 pKi = 9.7 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 293 2 1 3 3.8 CC(N)Cc1c2ccoc2c(Br)c2ccoc12 10.1021/jm9803525
9953185 207596 4 None 1 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to human 5-HT2B assessed as inhibition constantBinding affinity to human 5-HT2B assessed as inhibition constant
ChEMBL 370 4 2 3 4.6 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Cl)c1OC 10.1021/acs.jmedchem.2c00633
CHEMBL95121 207596 4 None 1 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to human 5-HT2B assessed as inhibition constantBinding affinity to human 5-HT2B assessed as inhibition constant
ChEMBL 370 4 2 3 4.6 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Cl)c1OC 10.1021/acs.jmedchem.2c00633
10597927 207508 0 None 93 2 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 414 4 2 3 4.7 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Br)c1OC 10.1021/acs.jmedchem.0c01887
CHEMBL94644 207508 0 None 93 2 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 414 4 2 3 4.7 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Br)c1OC 10.1021/acs.jmedchem.0c01887
10618362 207511 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 358 4 2 3 3.9 COc1ccc(CC2NCCc3c2[nH]c2c(F)cc(F)cc32)cc1OC 10.1021/acs.jmedchem.0c01887
CHEMBL94655 207511 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 358 4 2 3 3.9 COc1ccc(CC2NCCc3c2[nH]c2c(F)cc(F)cc32)cc1OC 10.1021/acs.jmedchem.0c01887
9953185 207596 4 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 370 4 2 3 4.6 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Cl)c1OC 10.1021/acs.jmedchem.0c01887
CHEMBL95121 207596 4 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 370 4 2 3 4.6 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)c(Cl)c1OC 10.1021/acs.jmedchem.0c01887
10760338 207823 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 350 4 2 3 4.2 COc1ccc(CC2NCCc3c2[nH]c2c(C)cc(C)cc32)cc1OC 10.1021/acs.jmedchem.0c01887
CHEMBL96427 207823 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 350 4 2 3 4.2 COc1ccc(CC2NCCc3c2[nH]c2c(C)cc(C)cc32)cc1OC 10.1021/acs.jmedchem.0c01887
10569875 207839 0 None 15 2 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 350 4 2 3 4.2 COc1ccc(CC2NCCc3c2[nH]c2cc(C)c(C)cc32)cc1OC 10.1021/acs.jmedchem.0c01887
CHEMBL96480 207839 0 None 15 2 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 350 4 2 3 4.2 COc1ccc(CC2NCCc3c2[nH]c2cc(C)c(C)cc32)cc1OC 10.1021/acs.jmedchem.0c01887
133 2479 52 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2479 52 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2479 52 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2479 52 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2479 52 None -2 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
188 3366 80 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1021/acs.jmedchem.2c00633
196968 3366 80 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1021/acs.jmedchem.2c00633
CHEMBL473186 3366 80 None -1 6 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1021/acs.jmedchem.2c00633
70772974 191465 6 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysisBinding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysis
ChEMBL 369 3 2 3 3.8 Cc1c(C(=O)N2CCC(c3ncc[nH]3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL5193649 191465 6 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysisBinding affinity to human 5-HT2B assessed as inhibition constant in microplate beta scintillation counter analysis
ChEMBL 369 3 2 3 3.8 Cc1c(C(=O)N2CCC(c3ncc[nH]3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/acs.jmedchem.2c00633
134 2497 24 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2497 24 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2497 24 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2497 24 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2497 24 None -2 68 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
242 469 124 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
34 469 124 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795 469 124 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
CHEMBL1112 469 124 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
DB01238 469 124 None -1 52 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
11393666 192962 0 None 1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192962 0 None 1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192962 0 None 1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
11978813 718 79 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
5014 718 79 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
7672 718 79 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
CHEMBL2105760 718 79 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
DB09128 718 79 None -2 24 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 10.1016/j.ejmech.2019.111736
11465618 102371 23 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 102371 23 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 102371 23 None -1 19 Human 9.4 pKi = 9.4 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
10686579 112336 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 312 2 2 1 4.8 c1ccc2c(CC3NCCc4c3[nH]c3ccccc43)cccc2c1 10.1021/acs.jmedchem.0c01887
CHEMBL329479 112336 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]-ketanserin from rat 5-HT2B expressed in mouse NIH/3T3 cells assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 312 2 2 1 4.8 c1ccc2c(CC3NCCc4c3[nH]c3ccccc43)cccc2c1 10.1021/acs.jmedchem.0c01887
23151734 103931 0 None 467 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 265 1 2 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(=O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092758 103931 0 None 467 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 265 1 2 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(=O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
11687730 120559 0 None 9 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 277 1 2 1 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343668 120559 0 None 9 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 277 1 2 1 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545816 120559 0 None 9 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 277 1 2 1 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
71528206 86942 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323581 86942 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 314 3 0 4 2.8 COC(OC)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
56597938 3909 3 None 2 9 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
7651 3909 3 None 2 9 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
CHEMBL2165126 3909 3 None 2 9 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm300603y
56597090 81954 0 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 7 0 4 6.6 Clc1cccc(C2CCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
CHEMBL2165137 81954 0 None -1 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 7 0 4 6.6 Clc1cccc(C2CCN(CCCCOc3ccc4scnc4c3)CC2)c1Cl 10.1021/jm300603y
56597938 3909 3 None 2 9 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 3909 3 None 2 9 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 3909 3 None 2 9 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
118706290 120507 0 None 128 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1C(O)c1cc(C(=O)N=C(N)N)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310116 120507 0 None 128 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1C(O)c1cc(C(=O)N=C(N)N)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545468 120507 0 None 128 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1C(O)c1cc(C(=O)N=C(N)N)ccc1-2 10.1016/j.bmc.2014.05.027
118706734 120500 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 309 2 3 2 1.9 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3310714 120500 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 309 2 3 2 1.9 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3545444 120500 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 309 2 3 2 1.9 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
150 2492 21 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
1764 2492 21 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
8226 2492 21 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
CHEMBL1201356 2492 21 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
DB00353 2492 21 None 1 16 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1021/jm100600y
118706282 120504 0 None 17 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3310111 120504 0 None 17 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3545465 120504 0 None 17 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.5 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
118706299 120511 0 None 64 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 269 1 3 2 2.3 N=C(N)NC(=O)c1ccc2c(c1)C(F)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310121 120511 0 None 64 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 269 1 3 2 2.3 N=C(N)NC(=O)c1ccc2c(c1)C(F)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545472 120511 0 None 64 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 269 1 3 2 2.3 N=C(N)NC(=O)c1ccc2c(c1)C(F)c1ccccc1-2 10.1016/j.bmc.2014.05.027
118706284 120498 0 None 31 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 285 1 3 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(F)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310112 120498 0 None 31 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 285 1 3 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(F)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545440 120498 0 None 31 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 285 1 3 2 1.3 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(F)c1-2 10.1016/j.bmc.2014.05.027
150 2492 21 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2492 21 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2492 21 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2492 21 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2492 21 None 1 16 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
71528205 86941 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323580 86941 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 368 5 1 4 2.2 CN(C)CCCNC(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
71528204 86940 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323579 86940 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
11358099 180382 0 None 3 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 3 1 4 2.8 COc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4752099 180382 0 None 3 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 3 1 4 2.8 COc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
11460460 182338 0 None -1 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.5 CC(C)n1nc2c(c1-c1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4784845 182338 0 None -1 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.5 CC(C)n1nc2c(c1-c1ccc(Cl)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
9954003 71671 24 None -1 9 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
CHEMBL196514 71671 24 None -1 9 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
16062782 97805 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 307 2 1 3 3.8 Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL272082 97805 0 None 2 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 307 2 1 3 3.8 Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
59757163 106315 0 None 218 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092760 106315 0 None 218 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139189 106315 0 None 218 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
118706732 120501 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 1 3 2 1.6 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3310713 120501 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 1 3 2 1.6 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
CHEMBL3545445 120501 0 None 3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 1 3 2 1.6 Cc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2(C)O 10.1016/j.bmc.2014.05.027
56593482 3910 3 None 1 9 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 3910 3 None 1 9 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 3910 3 None 1 9 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
10568771 102762 2 None -5 5 Human 8.9 pKi = 8.9 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL305275 102762 2 None -5 5 Human 8.9 pKi = 8.9 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL6710 102762 2 None -5 5 Human 8.9 pKi = 8.9 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]rauwolscine as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
242 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
34 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
60795 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
CHEMBL1112 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
DB01238 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
11658860 2329 51 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
2941 2329 51 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
4374 2329 51 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
CHEMBL360328 2329 51 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
DB04871 2329 51 None -1 3 Human 8.9 pKi = 8.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2012.10.091
37 775 60 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
460 775 60 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
54746 775 60 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
CHEMBL1201087 775 60 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
DB00248 775 60 None 1 17 Human 8.9 pKi = 8.9 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1021/ml3003814
242 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 469 124 None -1 52 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
118706278 120497 0 None 26 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(Cl)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310109 120497 0 None 26 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(Cl)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545439 120497 0 None 26 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(Cl)c1-2 10.1016/j.bmc.2014.05.027
2865 4112 73 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
59 4112 73 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
60854 4112 73 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
CHEMBL708 4112 73 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
DB00246 4112 73 None -12 54 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
9888211 21384 13 None -1 10 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 21384 13 None -1 10 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
10568771 102762 2 None -5 5 Human 8.8 pKi = 8.8 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL305275 102762 2 None -5 5 Human 8.8 pKi = 8.8 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
CHEMBL6710 102762 2 None -5 5 Human 8.8 pKi = 8.8 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 297 2 1 3 2.2 C[C@@H](N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm980076u
10017554 4309 29 None -1 4 Human 8.8 pKi = 8.8 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm9803525
CHEMBL101008 4309 29 None -1 4 Human 8.8 pKi = 8.8 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 297 2 1 3 2.2 CC(N)Cc1c2c(c(Br)c3c1OCC3)OCC2 10.1021/jm9803525
11957541 1446 40 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
1229 1446 40 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
147 1446 40 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
170617 1446 40 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
CHEMBL6616 1446 40 None -2 16 Human 8.8 pKi = 8.8 Binding
Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/acs.jmedchem.6b01422
118706285 112861 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 2 3 2 1.7 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3310113 112861 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 295 2 3 2 1.7 CCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
135399866 72026 2 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
CHEMBL197653 72026 2 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 209 2 2 4 1.2 C[C@H](N)Cn1ncc2ccc(O)c(F)c21 10.1021/jm050663x
118464429 167093 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4290245 167093 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 383 1 3 5 2.6 NC1=NC2(CCCCC2)NC(Nc2cccc(I)c2)=N1 10.1021/acsmedchemlett.8b00300
127048333 140655 1 None 38 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815112 140655 1 None 38 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccccc2F)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
118706280 120503 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cc(Cl)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310110 120503 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cc(Cl)ccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545464 120503 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cc(Cl)ccc1-2 10.1016/j.bmc.2014.05.027
118717220 120554 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343669 120554 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545811 120554 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 305 1 2 1 2.9 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
72734860 103930 0 None 6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092753 103930 0 None 6 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmc.2013.10.010
11277147 106314 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092759 106314 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139188 106314 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
11277147 106314 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3092759 106314 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3139188 106314 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2014.05.027
134 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
1775 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
9681 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
CHEMBL1065 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
DB00247 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.ejmech.2019.111736
206 2476 16 None -1 25 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/S0960-894X(96)00503-3
68848 2476 16 None -1 25 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/S0960-894X(96)00503-3
CHEMBL12314 2476 16 None -1 25 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/S0960-894X(96)00503-3
192 3476 54 None -10 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10.1021/jm990388c
443390 3476 54 None -10 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10.1021/jm990388c
CHEMBL14276 3476 54 None -10 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10.1021/jm990388c
10573762 98755 0 None 1 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)cc1)CC2 10.1021/jm990388c
CHEMBL278267 98755 0 None 1 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)cc1)CC2 10.1021/jm990388c
10670813 162567 0 None -15 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 4 1 3 5.9 CCc1cc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc(-c2cccnc2)c1 10.1021/jm990388c
CHEMBL416896 162567 0 None -15 3 Human 8.0 pKi = 8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 4 1 3 5.9 CCc1cc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc(-c2cccnc2)c1 10.1021/jm990388c
44397929 67151 0 None -6 3 Human 8.0 pKi = 8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL187739 67151 0 None -6 3 Human 8.0 pKi = 8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
10808965 100303 0 None -3 3 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 367 3 1 3 4.8 CCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL289436 100303 0 None -3 3 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 367 3 1 3 4.8 CCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
46230098 199306 0 None -3 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590580 199306 0 None -3 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1cccc2c1C(=O)NC1CCNCCN21 10.1016/j.bmcl.2009.12.014
18931422 207369 0 None -50 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 435 8 2 5 3.4 COc1ccc(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL93862 207369 0 None -50 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 435 8 2 5 3.4 COc1ccc(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
10740494 35109 0 None -12 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14345 35109 0 None -12 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cccnc3)c1)CC2 10.1021/jm990388c
10764263 40856 0 None -15 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccncc3)c1)CC2 10.1021/jm990388c
CHEMBL14863 40856 0 None -15 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccncc3)c1)CC2 10.1021/jm990388c
10740495 98601 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)nc1)CC2 10.1021/jm990388c
CHEMBL277111 98601 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 414 3 1 4 4.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3cccnc3)nc1)CC2 10.1021/jm990388c
122178705 121345 0 None 2 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581250 121345 0 None 2 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
59395105 106313 1 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 252 1 3 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3092755 106313 1 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 252 1 3 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3139187 106313 1 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 252 1 3 1 1.7 NC(N)=NC(=O)c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmc.2013.10.010
118729272 120684 0 None 3 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402680 120684 0 None 3 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547158 120684 0 None 3 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
44214724 194963 0 None -19 3 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cnccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL54707 194963 0 None -19 3 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cnccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
5 139 72 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
5202 139 72 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
CHEMBL39 139 72 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
DB08839 139 72 None -13 55 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.1c00726
24841480 183875 0 None -50 20 Human 7.0 pKi = 7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183875 0 None -50 20 Human 7.0 pKi = 7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
193 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
3644637 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
CHEMBL14563 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
194 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
443391 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
CHEMBL14460 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm990388c
193 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
3644637 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
CHEMBL14563 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
194 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
443391 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
CHEMBL14460 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2005.08.004
CHEMBL5285512 194276 0 None 1 3 Human 7.0 pKi = 7 Binding
Binding affinity to 5-HT2BR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2BR (unknown origin) assessed as inhibition constant
ChEMBL 327 2 1 3 4.9 COc1ccc2[nH]c3c(-c4cn(C)c5ccccc45)nccc3c2c1 10.1021/acs.jmedchem.0c01887
193 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
3644637 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
CHEMBL14563 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
194 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
443391 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
CHEMBL14460 3481 31 None -100 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/s0960-894x(00)00364-4
44298230 194579 0 None -79 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 492 3 1 4 6.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)c(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL53152 194579 0 None -79 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 492 3 1 4 6.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)c(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
44298022 195535 0 None -63 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 5 1 4 5.8 CCCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55472 195535 0 None -63 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 5 1 4 5.8 CCCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
18931133 168007 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 465 9 2 6 3.4 COc1cc(OC)c(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL432217 168007 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 465 9 2 6 3.4 COc1cc(OC)c(-c2ccccc2)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
145977338 163693 0 None 19 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 259 3 2 4 2.2 Oc1ccccc1C1=NC(Cc2c[nH]cn2)CS1 10.1021/acs.jnatprod.7b00317
CHEMBL4205064 163693 0 None 19 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 259 3 2 4 2.2 Oc1ccccc1C1=NC(Cc2c[nH]cn2)CS1 10.1021/acs.jnatprod.7b00317
145963830 164099 0 None 7 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 164099 0 None 7 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
193 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm970424c
3644637 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm970424c
CHEMBL14563 3480 46 None -707 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 10.1021/jm970424c
11419526 88027 0 None -100 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3ccc(Cl)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234533 88027 0 None -100 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3ccc(Cl)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
16215237 88146 0 None -39 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(Cl)c(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234738 88146 0 None -39 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(Cl)c(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10503674 98797 0 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3c(F)cccc3F)c1)CC2 10.1021/jm990388c
CHEMBL278685 98797 0 None -3 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3c(F)cccc3F)c1)CC2 10.1021/jm990388c
9813197 96506 6 None -11 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 1 1 2.7 Clc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL262862 96506 6 None -11 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 1 1 2.7 Clc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
25122651 200226 0 None -23 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL597002 200226 0 None -23 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
67268994 163944 2 None -3 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 163944 2 None -3 7 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
44298108 100897 0 None -39 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL293937 100897 0 None -39 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
44298092 101942 0 None -19 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 400 4 1 5 4.7 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccs3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL301409 101942 0 None -19 2 Human 7.0 pKi = 7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 400 4 1 5 4.7 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccs3)nc1)CC2 10.1016/s0960-894x(00)00365-6
162663486 181975 0 None - 1 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2cccc(C(F)(F)F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4780527 181975 0 None - 1 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2cccc(C(F)(F)F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
162672422 183157 0 None -1 2 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
CHEMBL4795598 183157 0 None -1 2 Human 6.0 pKi = 6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
24888181 80095 0 None -158 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL213272 80095 0 None -158 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
24887525 80340 1 None -199 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(C)(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL214398 80340 1 None -199 3 Human 6.0 pKi = 6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(C)(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
9888494 98143 0 None -446 13 Human 6.0 pKi = 6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determinedBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273921 98143 0 None -446 13 Human 6.0 pKi = 6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determinedBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
11168182 3508 25 None -158 13 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3508 25 None -158 13 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3508 25 None -158 13 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
6918648 101532 1 None -1621 14 Human 6.0 pKi = 6 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL29846 101532 1 None -1621 14 Human 6.0 pKi = 6 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
145972374 164650 0 None -3 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
CHEMBL4216860 164650 0 None -3 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
136054961 57289 4 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
CHEMBL1651091 57289 4 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
153287535 174876 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 0 1 3 2.0 CN1CC[C@H]2c3ccc(O)cc3OC[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4564308 174876 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 0 1 3 2.0 CN1CC[C@H]2c3ccc(O)cc3OC[C@]21C 10.1021/acsmedchemlett.9b00225
23462894 157207 3 None -15 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 240 1 0 3 2.3 CN1CCc2ccc([N+](=O)[O-])c(Cl)c2CC1 10.1016/j.bmc.2007.12.009
CHEMBL407636 157207 3 None -15 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 240 1 0 3 2.3 CN1CCc2ccc([N+](=O)[O-])c(Cl)c2CC1 10.1016/j.bmc.2007.12.009
9934284 90267 0 None -2511 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238520 90267 0 None -2511 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
76325517 105705 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 272 3 1 4 3.3 O=c1cc(CCc2cccs2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3126302 105705 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 272 3 1 4 3.3 O=c1cc(CCc2cccs2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
118278480 121985 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2ccc(O)cc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593950 121985 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2ccc(O)cc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
44453877 155592 0 None -19 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 305 2 1 3 3.6 Fc1ccc(-c2nc(-c3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL404582 155592 0 None -19 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 305 2 1 3 3.6 Fc1ccc(-c2nc(-c3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
44298151 100838 0 None -31 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Cl)ccc21 10.1016/s0960-894x(00)00365-6
CHEMBL293597 100838 0 None -31 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Cl)ccc21 10.1016/s0960-894x(00)00365-6
44298158 193950 0 None -12 3 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(00)00365-6
CHEMBL52783 193950 0 None -12 3 Human 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 380 4 1 4 4.3 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(00)00365-6
6918648 101532 1 None -1621 14 Human 6.0 pKi = 6 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
CHEMBL29846 101532 1 None -1621 14 Human 6.0 pKi = 6 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
3233 3486 44 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3486 44 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3486 44 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3486 44 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3486 44 None -165 12 Human 5.0 pKi = 5 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
16063047 95354 0 None -77 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL256811 95354 0 None -77 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCCC3)cc1 10.1016/j.bmcl.2008.01.090
122483292 138086 0 None -3 7 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764335 138086 0 None -3 7 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765876 138086 0 None -3 7 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
141 1415 35 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
6089 1415 35 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
CHEMBL12420 1415 35 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
DB01488 1415 35 None -1 22 Human 7.0 pKi = 7 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/jm980692q
136054961 57289 4 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/np100588c
CHEMBL1651091 57289 4 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 220 2 2 4 1.6 NC(=O)c1csc(-c2ccccc2O)n1 10.1021/np100588c
73213196 104433 4 None 1 13 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
CHEMBL3104093 104433 4 None 1 13 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2014.05.016
73213196 104433 4 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104433 4 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
73213196 104433 4 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104433 4 None 1 13 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
142601343 185579 0 None -36 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 185579 0 None -36 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
71455083 81801 0 None -173 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 81801 0 None -173 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
2520 203985 70 None -4 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 203985 70 None -4 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 203985 70 None -4 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
118055295 178048 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 242 0 1 2 2.2 FC(F)(F)c1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4647417 178048 0 None -17 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 242 0 1 2 2.2 FC(F)(F)c1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
11324968 91056 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397880 91056 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
168285382 191496 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5194057 191496 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
44582707 186974 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 430 10 0 6 4.1 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490634 186974 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 430 10 0 6 4.1 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
13091359 113512 0 None -1479 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 113512 0 None -1479 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
53251189 130868 6 None - 1 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2B
ChEMBL 452 5 3 7 5.1 Cc1cc(Nc2nccc(C)n2)cc(-c2cnc([C@@]3(O)CC[C@H](C(=O)O)C(C)(C)C3)s2)c1 10.6019/CHEMBL5212743
CHEMBL3685796 130868 6 None - 1 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000704a HTR2B
ChEMBL 452 5 3 7 5.1 Cc1cc(Nc2nccc(C)n2)cc(-c2cnc([C@@]3(O)CC[C@H](C(=O)O)C(C)(C)C3)s2)c1 10.6019/CHEMBL5212743
135367405 164172 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 164172 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
122179556 121462 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2B
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 10.6019/CHEMBL5212743
CHEMBL3582461 121462 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR2B
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 10.6019/CHEMBL5212743
15560577 185317 9 None 1 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4859858 185317 9 None 1 10 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
123683 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
422 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
CHEMBL119709 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
DB05511 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screeningBinding affinity to 5HT2B receptor (unknown origin) by PDSP screening
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm501021n
123683 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
422 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
CHEMBL119709 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
DB05511 3099 63 None -12302 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
16115652 83462 0 None -27 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL220211 83462 0 None -27 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 1 3 1.8 COc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
71061724 145527 0 None 1 5 Mouse 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL3915107 145527 0 None 1 5 Mouse 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10660 14384 58 None -29 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14384 58 None -29 12 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
134138168 147666 0 None 1 10 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147666 0 None 1 10 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
44397832 123083 0 None -7 3 Human 8.0 pKi = 8.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 256 0 1 2 2.4 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)cc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL361079 123083 0 None -7 3 Human 8.0 pKi = 8.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 256 0 1 2 2.4 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)cc3N12 10.1016/j.bmcl.2005.05.074
118706287 120505 0 None 14 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccc(Cl)cc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310114 120505 0 None 14 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccc(Cl)cc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545466 120505 0 None 14 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 301 1 3 2 1.8 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1ccc(Cl)cc1-2 10.1016/j.bmc.2014.05.027
10131066 21571 0 None -4 3 Human 8.0 pKi = 8.0 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 2 1 3 2.4 CC(N)Cc1cn(C)c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL131736 21571 0 None -4 3 Human 8.0 pKi = 8.0 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 2 1 3 2.4 CC(N)Cc1cn(C)c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL5286886 194338 0 None 7 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 405 6 4 8 1.4 OC[C@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1039/D1MD00167A
134141831 146662 0 None 2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3923870 146662 0 None 2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 6 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
45486902 196923 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL566396 196923 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
118729270 120676 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402678 120676 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547139 120676 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
145965628 164023 0 None -4 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4208914 164023 0 None -4 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
146025727 171661 0 None -40 27 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171661 0 None -40 27 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
132060743 162212 0 None -4 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 162212 0 None -4 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
10541003 103092 0 None -2 3 Human 5.0 pKi = 5.0 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@H]3CO2 10.1021/jm980076u
CHEMBL307770 103092 0 None -2 3 Human 5.0 pKi = 5.0 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@H]3CO2 10.1021/jm980076u
136118640 76289 0 None 3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058700 76289 0 None 3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
21044391 76602 0 None -21 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 2 4 0.3 C[C@@H]1CNC[C@H]2Cc3ccc(CO)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL206386 76602 0 None -21 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 2 4 0.3 C[C@@H]1CNC[C@H]2Cc3ccc(CO)nc3N12 10.1016/j.bmcl.2005.11.083
2333 142310 97 None 1 2 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
CHEMBL388590 142310 97 None 1 2 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 nan
11313985 91054 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397878 91054 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
18715561 73015 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201062 73015 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cccnc3c21 10.1016/j.bmcl.2005.10.029
46914774 15410 0 None 21 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1215037 15410 0 None 21 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
16115269 138104 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL376676 138104 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
21786603 134838 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 259 3 2 3 1.7 CN1CCN(CCc2c[nH]c3cccc(O)c23)CC1 10.1016/j.bmcl.2005.06.104
CHEMBL371899 134838 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 259 3 2 3 1.7 CN1CCN(CCc2c[nH]c3cccc(O)c23)CC1 10.1016/j.bmcl.2005.06.104
127051592 140853 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140853 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140853 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
2771 194994 74 None 1 27 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 194994 74 None 1 27 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 194994 74 None 1 27 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
127051592 140853 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140853 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140853 0 None -51 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
104903 56314 17 None -4 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56314 17 None -4 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
58911534 91080 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397904 91080 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
2723 154022 108 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
CHEMBL398440 154022 108 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl nan
1379258 67766 13 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909050 67766 13 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 3 0 1 4.1 Cc1ccccc1C(=O)N1CCC(Cc2ccccc2)CC1 nan
16754 85545 50 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL228082 85545 50 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
5 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
5202 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL39 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
DB08839 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL5081379 214723 0 None -1 9 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
58405183 110670 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 339 6 1 3 3.9 FC(F)(COc1ccc(Cl)cc1OC1CNC1)c1ccccc1 10.1021/ml500082j
CHEMBL3260336 110670 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 339 6 1 3 3.9 FC(F)(COc1ccc(Cl)cc1OC1CNC1)c1ccccc1 10.1021/ml500082j
11380477 179658 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 280 2 1 4 2.7 CC(C)n1nc2c(c1-c1ccc(C#N)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4743582 179658 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 280 2 1 4 2.7 CC(C)n1nc2c(c1-c1ccc(C#N)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
5 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
5202 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
CHEMBL39 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
DB08839 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2005.10.029
10198431 73876 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201930 73876 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
189 3466 39 None -5 17 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
5163 3466 39 None -5 17 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
CHEMBL297784 3466 39 None -5 17 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
11625624 113061 0 None -17 7 Human 7.9 pKi = 7.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL331291 113061 0 None -17 7 Human 7.9 pKi = 7.9 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
189 3466 39 None -5 17 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
5163 3466 39 None -5 17 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
CHEMBL297784 3466 39 None -5 17 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1016/j.bmcl.2013.12.024
10741816 98162 0 None -5 3 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3c(C)ccnc3C)c1)CC2 10.1021/jm990388c
CHEMBL274066 98162 0 None -5 3 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3c(C)ccnc3C)c1)CC2 10.1021/jm990388c
10549658 98255 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3ccncc3)cc1)CC2 10.1021/jm990388c
CHEMBL274692 98255 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(-c3ccncc3)cc1)CC2 10.1021/jm990388c
18475509 101920 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 3 3.9 CN1CCc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
CHEMBL301209 101920 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 3 3.9 CN1CCc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
191 3472 52 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970741j
443389 3472 52 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970741j
CHEMBL276140 3472 52 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970741j
44298172 101744 0 None -6 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cncnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL299938 101744 0 None -6 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cncnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298163 195378 0 None -25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL55207 195378 0 None -25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
191 3472 52 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970424c
443389 3472 52 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970424c
CHEMBL276140 3472 52 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 10.1021/jm970424c
9887537 84316 43 None -15 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL221692 84316 43 None -15 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL4751170 84316 43 None -15 9 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
44298246 195586 0 None -2 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 397 4 1 5 4.0 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55597 195586 0 None -2 3 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 397 4 1 5 4.0 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3nccn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
56658155 65633 0 None 13 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccccc1CCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
CHEMBL1834252 65633 0 None 13 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccccc1CCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
145972796 164572 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 236 3 2 4 2.0 CNc1ccccc1C1=N[C@@H](CO)[C@H](C)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4215741 164572 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 236 3 2 4 2.0 CNc1ccccc1C1=N[C@@H](CO)[C@H](C)S1 10.1021/acs.jnatprod.7b00317
71212556 143537 0 None -24 6 Human 6.9 pKi = 6.9 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
CHEMBL3899169 143537 0 None -24 6 Human 6.9 pKi = 6.9 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
155561439 175642 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 411 4 4 7 3.5 Oc1ccc(CCNc2nc(C#Cc3ccc(Cl)s3)nc3[nH]cnc23)cc1O 10.1039/C8MD00317C
CHEMBL4581568 175642 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 411 4 4 7 3.5 Oc1ccc(CCNc2nc(C#Cc3ccc(Cl)s3)nc3[nH]cnc23)cc1O 10.1039/C8MD00317C
44404899 70403 2 None -70 4 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 190 2 2 2 1.9 CN(C)Cc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL194588 70403 2 None -70 4 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 190 2 2 2 1.9 CN(C)Cc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
44404904 132986 1 None -11 3 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 2 1 3 1.9 CN(C)Cc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL370221 132986 1 None -11 3 Human 5.9 pKi = 5.9 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 2 1 3 1.9 CN(C)Cc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
127050699 140847 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819082 140847 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819726 140847 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
117209918 186386 1 None -3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4876036 186386 1 None -3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
135508617 136016503 10598 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL1170237 10598 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
9869628 72014 0 None -199 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 440 7 0 4 4.8 COc1cc2c(cc1OCCN1CCCCC1)N(C(=O)/C=C/c1ccccc1Cl)CC2 10.1016/j.bmcl.2005.08.004
CHEMBL197630 72014 0 None -199 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 440 7 0 4 4.8 COc1cc2c(cc1OCCN1CCCCC1)N(C(=O)/C=C/c1ccccc1Cl)CC2 10.1016/j.bmcl.2005.08.004
10127968 72190 0 None -15 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 479 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198109 72190 0 None -15 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 479 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
10479409 78034 0 None -25 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(C2=CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL210007 78034 0 None -25 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(C2=CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
49850874 56432 0 None -398 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632210 56432 0 None -398 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
44298243 100634 0 None -100 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
CHEMBL292228 100634 0 None -100 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
44298254 194512 0 None -50 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 442 4 1 4 5.8 CCc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL52919 194512 0 None -50 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 442 4 1 4 5.8 CCc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
22619858 199051 1 None -39 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL58765 199051 1 None -39 3 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
18931348 104714 0 None -39 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 389 8 2 6 1.7 COc1ccc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)c1 10.1016/S0960-894X(96)00503-3
CHEMBL310656 104714 0 None -39 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 389 8 2 6 1.7 COc1ccc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)c1 10.1016/S0960-894X(96)00503-3
44324011 111584 0 None -12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 562 11 3 8 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(F)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL328375 111584 0 None -12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 562 11 3 8 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(F)cc1 10.1016/S0960-894X(96)00503-3
148302367 173497 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 2 1 2 4.0 CC[C@H]1c2cc(-c3ccccc3)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4530979 173497 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 2 1 2 4.0 CC[C@H]1c2cc(-c3ccccc3)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
149396365 175980 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 295 3 1 3 3.5 C[C@@]12COc3cc(OCc4ccccc4)ccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4589450 175980 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 295 3 1 3 3.5 C[C@@]12COc3cc(OCc4ccccc4)ccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
44430976 88012 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCC(C)C1 10.1016/j.bmcl.2006.10.029
CHEMBL234492 88012 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCC(C)C1 10.1016/j.bmcl.2006.10.029
11236301 88025 0 None -63 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 450 6 0 4 4.9 COc1ccc(N2Cc3c(F)c(F)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234531 88025 0 None -63 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 450 6 0 4 4.9 COc1ccc(N2Cc3c(F)c(F)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11475519 152051 0 None -79 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 414 6 0 4 4.6 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL396747 152051 0 None -79 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 414 6 0 4 4.6 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
44430979 153168 0 None -19 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.8 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1[C@@H](C)CCC[C@H]1C 10.1016/j.bmcl.2006.10.029
CHEMBL397709 153168 0 None -19 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.8 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1[C@@H](C)CCC[C@H]1C 10.1016/j.bmcl.2006.10.029
162654275 180656 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4755344 180656 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 310 5 1 4 3.7 COc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
10287730 3510 40 None -1584 12 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor Binding affinity for human 5-hydroxytryptamine 2B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 3510 40 None -1584 12 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor Binding affinity for human 5-hydroxytryptamine 2B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 3510 40 None -1584 12 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor Binding affinity for human 5-hydroxytryptamine 2B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
10217208 72184 0 None -125 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3cccc(Cl)c3Cl)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198097 72184 0 None -125 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3cccc(Cl)c3Cl)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
44404608 72223 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 346 6 1 4 2.7 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCO 10.1016/j.bmcl.2005.08.004
CHEMBL198192 72223 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 346 6 1 4 2.7 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCO 10.1016/j.bmcl.2005.08.004
10309622 141349 0 None -1000 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 395 7 0 4 4.0 COc1ccc(N2CCN(c3ccccc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL383800 141349 0 None -1000 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 395 7 0 4 4.0 COc1ccc(N2CCN(c3ccccc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
44414209 81207 0 None -398 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 424 7 0 4 4.4 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL215864 81207 0 None -398 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 424 7 0 4 4.4 COc1ccc(N2CC=C(c3ccc(F)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
9891002 107381 0 None -1258 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligandBinding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 107381 0 None -1258 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligandBinding affinity to human cloned 5-HT2B receptor in HEK 293 cells using [3H]- -5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
11304596 56366 0 None -7943 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631542 56366 0 None -7943 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
9827938 11739 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11739 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11739 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
2470 3626 50 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
3300 3626 50 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
5265 3626 50 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
99 3626 50 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
CHEMBL267930 3626 50 None -14125 60 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/S0960-894X(96)00503-3
10008294 206804 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 574 12 3 9 2.5 COc1ccc(S(=O)(=O)Nc2cc(C(=O)CCCCN3CCC4(CC3)NC(=O)NC4=O)c(OC)cc2OC)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90467 206804 0 None -63 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 574 12 3 9 2.5 COc1ccc(S(=O)(=O)Nc2cc(C(=O)CCCCN3CCC4(CC3)NC(=O)NC4=O)c(OC)cc2OC)cc1 10.1016/S0960-894X(96)00503-3
10371119 206984 0 None -794 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 8 3.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)C)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL91454 206984 0 None -794 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 8 3.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)C)cc1 10.1016/S0960-894X(96)00503-3
127050699 140847 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819082 140847 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819726 140847 0 None -14 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
122182283 121984 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2cccc(O)c2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593949 121984 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 3 2 4 3.0 O=c1cc(CCc2cccc(O)c2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
9935387 99414 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL282971 99414 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
9913554 100965 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 100965 0 None -1584 14 Human 5.9 pKi = 5.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
136030693 57290 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/np100588c
CHEMBL1651092 57290 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/np100588c
13149 2528 36 None -20 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.1c00726
3034396 2528 36 None -20 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.1c00726
CHEMBL299031 2528 36 None -20 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@@H]1CN2CCC3=C([C@@H]2C[C@@H]1/C(=C\OC)/C(=O)OC)NC4=C3C(=CC=C4)OC 10.1021/acs.jmedchem.1c00726
1201549 594 24 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 594 24 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 594 24 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 594 24 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 594 24 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 594 24 None -26 20 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
118055293 177221 0 None -17 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 252 0 1 2 1.9 Brc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4635854 177221 0 None -17 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 252 0 1 2 1.9 Brc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
58911604 91077 1 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2ccc(Cl)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397901 91077 1 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2ccc(Cl)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
135846982 93026 0 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cc(Br)ccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442268 93026 0 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cc(Br)ccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
5510 205829 100 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
CHEMBL83668 205829 100 None - 1 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 nan
135846955 189459 4 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)N/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL513803 189459 4 None 7 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)N/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
4122 207602 108 None -3 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
CHEMBL9514 207602 108 None -3 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 301 3 2 5 3.0 COC(=O)Nc1nc2ccc(C(=O)c3cccs3)cc2[nH]1 nan
71682216 91085 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 260 3 1 3 1.4 CCCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397909 91085 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 260 3 1 3 1.4 CCCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL4754103 214016 0 None - 1 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000328a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000328a HTR2B
ChEMBL None None None CNC(=O)Nc1ccc2c(c1)CC[C@]21OC(=O)N(CC(=O)N(Cc2ccc(F)cc2)[C@@H](C)C(F)(F)F)C1=O 10.6019/CHEMBL5212743
92042876 151312 0 None -2 10 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151312 0 None -2 10 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
9920815 67219 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL188033 67219 0 None -7 3 Human 7.9 pKi = 7.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
5 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
5202 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
CHEMBL39 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
DB08839 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050663x
152 363 29 None 1 19 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
2107 363 29 None 1 19 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
CHEMBL275854 363 29 None 1 19 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm050663x
24826790 91065 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397889 91065 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
46230095 199268 0 None 11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 271 0 2 3 1.2 O=C1NC2CNCCN2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590333 199268 0 None 11 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 271 0 2 3 1.2 O=C1NC2CNCCN2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2009.12.014
127048336 140580 1 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2I)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813855 140580 1 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2I)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
5 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
5202 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
CHEMBL39 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
DB08839 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030205t
152 363 29 None 1 19 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
2107 363 29 None 1 19 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
CHEMBL275854 363 29 None 1 19 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm030205t
9856041 24082 3 None -3 8 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL133868 24082 3 None -3 8 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
5 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
5202 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
CHEMBL39 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
DB08839 139 72 None -13 55 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2014.02.029
156013985 177151 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter methodDisplacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter method
ChEMBL 230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23 10.1016/j.bmcl.2019.126929
CHEMBL4634785 177151 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter methodDisplacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in CHO cells measured after 120 mins by scintillation counter method
ChEMBL 230 0 1 2 1.8 C1=CC2CNCCN3C[C@@H]4CCC[C@@H]4C(=C1)C23 10.1016/j.bmcl.2019.126929
45486824 197354 0 None -14 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL569251 197354 0 None -14 3 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL5094234 215550 0 None -61 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 215550 0 None -61 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5090884 215554 0 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096072 215554 0 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
24771120 184076 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
CHEMBL482562 184076 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
136020618 163890 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4207302 163890 0 None 12 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
135753074 191084 9 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5187824 191084 9 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 341 4 2 5 2.2 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2ccccc2F)n1 10.1021/acs.jmedchem.1c01759
136030693 57290 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
CHEMBL1651092 57290 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 222 2 2 4 0.7 NC(=O)C1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
11739217 137015 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 300 2 1 3 2.2 CCOc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374660 137015 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 300 2 1 3 2.2 CCOc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
16063039 155591 0 None -147 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCCNC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL404581 155591 0 None -147 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.9 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCCNC3)cc1 10.1016/j.bmcl.2008.01.090
1353 1898 93 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1898 93 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1898 93 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1898 93 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1898 93 None -295 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL4537673 213966 29 None - 1 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000305b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000305b HTR2B
ChEMBL None None None C[C@H](c1ccnc(Nc2nc3ccc(-c4cc(N(C)C)ncn4)cc3[nH]2)c1)N1CCN(C(=O)CC(F)(F)F)CC1 10.6019/CHEMBL5212743
44409332 76701 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL206618 76701 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
162661262 181828 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 432 6 4 7 2.7 OC[C@@]12C[C@@H]1[C@@H](n1ccc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2020.127599
CHEMBL4778636 181828 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 432 6 4 7 2.7 OC[C@@]12C[C@@H]1[C@@H](n1ccc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2020.127599
1016 3720 78 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3720 78 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3720 78 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3720 78 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3720 78 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3720 78 None -17 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
71061585 160473 0 None 3 2 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4112090 160473 0 None 3 2 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL1909069 209053 0 None -1 3 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
117209971 186461 1 None -26 5 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4877051 186461 1 None -26 5 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
1343 1876 62 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
3519 1876 62 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
522 1876 62 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL862 1876 62 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
DB01018 1876 62 None -14 9 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N nan
CHEMBL4780458 214025 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000540a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000540a HTR2B
ChEMBL None None None O=C(Nc1cccnn1)N1CC(C/C=C/c2cncc(Oc3ccc(C(F)(F)F)cn3)n2)C1 10.6019/CHEMBL5212743
58911681 90956 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL2396668 90956 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
136118639 76288 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058699 76288 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
2337 3232 77 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3232 77 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3232 77 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3232 77 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3232 77 None -15 63 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
71455625 82935 0 None -3388 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181170 82935 0 None -3388 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 353 5 0 4 4.4 CCCN1CCC(COc2nc3c(F)cccc3c3ncccc23)CC1 10.1021/jm300943r
44407398 74389 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
CHEMBL202616 74389 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 365 5 1 3 5.5 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.10.029
136030596 57288 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/np100588c
CHEMBL1651090 57288 1 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/np100588c
168277287 190126 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 426 7 2 3 7.8 CCCC(CCC)c1nc2c(Nc3ccc(Cl)c(Cl)c3)nc3ccccc3c2[nH]1 10.1021/acs.jmedchem.2c01170
CHEMBL5173661 190126 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 426 7 2 3 7.8 CCCC(CCC)c1nc2c(Nc3ccc(Cl)c(Cl)c3)nc3ccccc3c2[nH]1 10.1021/acs.jmedchem.2c01170
25123011 201170 0 None -74 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
CHEMBL603483 201170 0 None -74 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
46230046 199224 0 None 14 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590077 199224 0 None 14 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 203 0 2 3 0.2 O=C1NC2CNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
135846958 76216 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058408 76216 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
18715555 74346 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
CHEMBL202458 74346 0 None -8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 359 5 1 5 4.1 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2005.10.029
168286940 192257 0 None -691 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysisDisplacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysis
ChEMBL 454 7 1 4 4.0 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5205903 192257 0 None -691 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysisDisplacement of [3H]-LSD from human 5-HT2B receptor at 25 uM incubated for 1 hr by microbeta2 beta-counter analysis
ChEMBL 454 7 1 4 4.0 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
76518514 113510 0 None -147 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321788 113510 0 None -147 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
58911582 91070 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397894 91070 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
59012632 87709 0 None 91 2 Human 7.9 pKi = 7.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 388 2 1 3 4.6 COc1ccc(-c2cc3c4c(c2)[C@@H]2CNCC[C@@H]2N4CCC3)c(C(F)(F)F)c1 10.1016/j.bmcl.2012.10.091
CHEMBL2337102 87709 0 None 91 2 Human 7.9 pKi = 7.9 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 388 2 1 3 4.6 COc1ccc(-c2cc3c4c(c2)[C@@H]2CNCC[C@@H]2N4CCC3)c(C(F)(F)F)c1 10.1016/j.bmcl.2012.10.091
127051482 140629 1 None 8 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccc(F)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814737 140629 1 None 8 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2ccc(F)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127050282 140648 1 None 7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2cccc(Br)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815066 140648 1 None 7 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2cccc(Br)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
10353268 97742 1 None -2 4 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 216 2 2 2 2.0 NCCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL27173 97742 1 None -2 4 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 216 2 2 2 2.0 NCCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
24893978 1007 9 None -35 8 Human 6.9 pKi = 6.9 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 1007 9 None -35 8 Human 6.9 pKi = 6.9 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 1007 9 None -35 8 Human 6.9 pKi = 6.9 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
10176869 166003 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL425545 166003 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 222 0 1 2 2.0 Cc1c(Cl)ccc2c1N1CCNC[C@@H]1C2 10.1016/j.bmcl.2005.05.074
11595191 89031 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337488 89031 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2364960 89031 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 298 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N(C)[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
854531 152970 30 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT2BR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2BR (unknown origin) assessed as inhibition constant
ChEMBL 244 1 1 1 4.4 c1ccc(-c2nccc3c2[nH]c2ccccc23)cc1 10.1021/acs.jmedchem.0c01887
CHEMBL3975325 152970 30 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT2BR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2BR (unknown origin) assessed as inhibition constant
ChEMBL 244 1 1 1 4.4 c1ccc(-c2nccc3c2[nH]c2ccccc23)cc1 10.1021/acs.jmedchem.0c01887
145978819 163857 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2cccs2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4206939 163857 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2cccs2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
145975226 163909 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
CHEMBL4207529 163909 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 388 6 3 7 1.3 COC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1N=C(c2ccccc2O)S[C@@H]1C 10.1021/acs.jnatprod.7b00317
145976983 163982 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4208376 163982 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 333 4 1 3 4.6 C[C@H]1SC(c2ccc(-c3ccccc3)cc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
136030596 57288 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
CHEMBL1651090 57288 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 209 2 2 4 1.2 OC[C@@H]1CSC(c2ccccc2O)=N1 10.1021/acs.jnatprod.7b00317
44537940 18742 0 None -18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1278001 18742 0 None -18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
16115513 136377 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL373531 136377 0 None -23 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
136118732 76217 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058409 76217 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
122187383 123004 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(CC1CC1)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609148 123004 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(CC1CC1)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
72549033 110666 0 None -660 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometryDisplacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometry
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
CHEMBL3260311 110666 0 None -660 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometryDisplacement of [125I]-R-O-DOI from human 5-HT2B receptor expressed in CHO-K1 cells by by liquid scintillation spectrometry
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
155536080 172090 0 None 2 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 172090 0 None 2 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
142601333 185739 0 None -63 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4866412 185739 0 None -63 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
71062646 149519 0 None -2398 13 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 149519 0 None -2398 13 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
56675412 65636 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 334 6 0 3 4.2 c1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834255 65636 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 334 6 0 3 4.2 c1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
134141050 147279 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.4 O=C(O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3928983 147279 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.4 O=C(O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
21302483 87710 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 246 0 1 3 2.4 c1cc2c3c(c1)[C@@H]1CNCC[C@@H]1N3CCCS2 10.1016/j.bmcl.2012.10.091
CHEMBL2337103 87710 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Agonist activity at 5-HT2B receptor (unknown origin)Agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 246 0 1 3 2.4 c1cc2c3c(c1)[C@@H]1CNCC[C@@H]1N3CCCS2 10.1016/j.bmcl.2012.10.091
CHEMBL5094680 215487 0 None 3 8 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
46914487 15378 0 None 144 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214830 15378 0 None 144 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL5288004 194381 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1039/D1MD00167A
71461603 78509 1 None -7 3 Human 7.8 pKi = 7.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL2112055 78509 1 None -7 3 Human 7.8 pKi = 7.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
2585 800 103 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 800 103 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 800 103 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 800 103 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 800 103 None -18 22 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2389 3306 118 None -66 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3306 118 None -66 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3306 118 None -66 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3306 118 None -66 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3306 118 None -66 68 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
135520431 72580 9 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL199385 72580 9 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 177 2 2 4 0.7 NCCn1ncc2ccc(O)cc21 10.1021/jm050663x
24873257 180232 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.2 c1ccc(-c2c3c(nn2-c2ccccc2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4750414 180232 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 289 2 1 3 3.2 c1ccc(-c2c3c(nn2-c2ccccc2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
168274008 190172 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5174366 190172 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
134143752 150625 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3955519 150625 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
134143752 150625 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL3955519 150625 0 None 3 5 Human 7.8 pKi = 7.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 447 7 3 9 1.9 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
24824726 161085 1 None -20 6 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human 5-HT2B receptorAntagonist activity at human 5-HT2B receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4060529 161085 1 None -20 6 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human 5-HT2B receptorAntagonist activity at human 5-HT2B receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4117079 161085 1 None -20 6 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human 5-HT2B receptorAntagonist activity at human 5-HT2B receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5282336 161085 1 None -20 6 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human 5-HT2B receptorAntagonist activity at human 5-HT2B receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286389 161085 1 None -20 6 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human 5-HT2B receptorAntagonist activity at human 5-HT2B receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
10550406 31923 0 None -3 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3C)c1)CC2 10.1021/jm990388c
CHEMBL14076 31923 0 None -3 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3C)c1)CC2 10.1021/jm990388c
10718089 98528 0 None -31 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 443 4 1 4 5.4 COc1ccc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc1-c1cccnc1 10.1021/jm990388c
CHEMBL276571 98528 0 None -31 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 443 4 1 4 5.4 COc1ccc(NC(=O)N2CCc3cc(OC)c(C(F)(F)F)cc32)cc1-c1cccnc1 10.1021/jm990388c
10767350 99014 0 None -6 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 489 4 1 3 7.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3ccccc3)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL280297 99014 0 None -6 3 Human 7.8 pKi = 7.8 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 489 4 1 3 7.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3ccccc3)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
18475610 196773 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 327 3 2 3 4.5 COc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1Cl 10.1016/s0960-894x(01)00343-2
CHEMBL56557 196773 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 327 3 2 3 4.5 COc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1Cl 10.1016/s0960-894x(01)00343-2
10714852 163126 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 381 4 1 3 5.2 CCCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL41792 163126 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 381 4 1 3 5.2 CCCSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
44298082 194941 0 None -3 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ncccc3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL54484 194941 0 None -3 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ncccc3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
118055289 177875 0 None -19 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.7 Cc1cc2c3c(c1Cl)C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4644872 177875 0 None -19 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.7 Cc1cc2c3c(c1Cl)C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
10421236 188709 1 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 226 1 3 4 1.9 Nc1nccc(-c2c[nH]c3cccc(O)c23)n1 10.1016/j.bmc.2011.08.033
CHEMBL50498 188709 1 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 226 1 3 4 1.9 Nc1nccc(-c2c[nH]c3cccc(O)c23)n1 10.1016/j.bmc.2011.08.033
135367857 164580 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164580 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL5280298 194036 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT2BR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2BR (unknown origin) assessed as inhibition constant
ChEMBL 294 1 1 1 5.5 c1ccc2cc(-c3nccc4c3[nH]c3ccccc34)ccc2c1 10.1021/acs.jmedchem.0c01887
145967795 164799 0 None 5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4218679 164799 0 None 5 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
136259032 164616 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 205 2 1 4 2.3 O=Cc1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
CHEMBL4216337 164616 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 205 2 1 4 2.3 O=Cc1csc(-c2ccccc2O)n1 10.1021/acs.jnatprod.7b00317
CHEMBL4802045 214036 6 None - 1 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CC[C@@H](Nc1c(C#N)c(-c2ccc(-c3cccc(C)c3F)cc2)nc2cnccc12)C(=O)O 10.6019/CHEMBL4800729
732268 138271 33 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770837 138271 33 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 257 1 3 5 2.0 NC1=NC2(CCCCC2)NC(Nc2ccccc2)=N1 10.1021/acsmedchemlett.8b00300
127051843 140726 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140726 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
1222 1651 49 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
3396 1651 49 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
85 1651 49 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
CHEMBL46516 1651 49 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
DB04842 1651 49 None -52 33 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm100600y
CHEMBL4802045 214036 6 None - 1 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CC[C@@H](Nc1c(C#N)c(-c2ccc(-c3cccc(C)c3F)cc2)nc2cnccc12)C(=O)O 10.6019/CHEMBL4800729
2398 951 62 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 951 62 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 951 62 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 951 62 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 951 62 None -3 29 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
127051843 140726 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140726 0 None -6 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
155543832 173187 0 None -134 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 451 6 3 7 3.4 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4522864 173187 0 None -134 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 451 6 3 7 3.4 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
11952353 199837 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
CHEMBL594469 199837 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 345 4 1 4 3.0 Fc1ccc(F)c(CO[C@H]2CCc3ccc(N4CCNCC4)nc32)c1 10.1016/j.bmcl.2009.10.112
168274751 190614 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5181312 190614 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
11302765 84219 4 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL221113 84219 4 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.4 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
10235 2656 1 None -61 6 Human 6.8 pKi = 6.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
137553161 2656 1 None -61 6 Human 6.8 pKi = 6.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
CHEMBL4470080 2656 1 None -61 6 Human 6.8 pKi = 6.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
CHEMBL4545807 213971 0 None - 1 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000748a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000748a HTR2B
ChEMBL None None None Cn1c(-c2csc(C3CCN(CC4=NC5N=CC=CC5N4)CC3)n2)nc2ccccc21 10.6019/CHEMBL5212743
56645363 121464 12 None -2 4 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2B
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 10.6019/CHEMBL5212743
CHEMBL3582478 121464 12 None -2 4 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000313b HTR2B
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 10.6019/CHEMBL5212743
136118650 76294 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058705 76294 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
44581972 175576 0 None -5 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458001 175576 0 None -5 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
136020620 57294 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 219 2 1 4 2.6 Cc1sc(-c2ccccc2O)nc1C=O 10.1021/np100588c
CHEMBL1651096 57294 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 219 2 1 4 2.6 Cc1sc(-c2ccccc2O)nc1C=O 10.1021/np100588c
142601325 185845 0 None -3 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4868035 185845 0 None -3 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
16117151 60057 0 None -154 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 60057 0 None -154 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 60057 0 None -154 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
25263297 184313 0 None -19 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
CHEMBL484345 184313 0 None -19 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
53483975 65584 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1833977 65584 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
1605 2327 117 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
3957 2327 117 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
7216 2327 117 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
CHEMBL998 2327 117 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
DB00455 2327 117 None -1 4 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
168282554 190842 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OC(C)C)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5184659 190842 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OC(C)C)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
155530292 171470 0 None -3548 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 458 5 4 8 1.6 O=C(NC1CC1)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4463802 171470 0 None -3548 7 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 458 5 4 8 1.6 O=C(NC1CC1)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
10151289 133558 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 434 6 0 4 4.7 O=C1N(c2ccc(OCCN3CCCCC3)nc2)CCN1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.08.004
CHEMBL371211 133558 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 434 6 0 4 4.7 O=C1N(c2ccc(OCCN3CCCCC3)nc2)CCN1c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.08.004
49850872 56428 0 None -630 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 388 5 1 4 3.9 CC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632206 56428 0 None -630 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 388 5 1 4 3.9 CC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
10830245 101397 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 329 1 1 2 4.6 CC(C)(C)c1cc2c(cc1Cl)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL297445 101397 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 329 1 1 2 4.6 CC(C)(C)c1cc2c(cc1Cl)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
10408409 193139 0 None -79 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL52308 193139 0 None -79 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C)nn1)CC2 10.1016/s0960-894x(00)00364-4
44298226 196462 0 None -100 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 378 3 1 4 4.6 Cc1cc2c(cc1F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL56336 196462 0 None -100 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 378 3 1 4 4.6 Cc1cc2c(cc1F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
153287542 169510 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3c(-c4ccccc4)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4435237 169510 0 None -6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3c(-c4ccccc4)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
11237290 87928 0 None -199 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 458 6 0 4 4.7 COc1ccc(N2Cc3cccc(Br)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234109 87928 0 None -199 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 458 6 0 4 4.7 COc1ccc(N2Cc3cccc(Br)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10413268 152643 0 None -31 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 453 6 0 5 4.9 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL397259 152643 0 None -31 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 453 6 0 5 4.9 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
44420682 137583 0 None -3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
CHEMBL375642 137583 0 None -3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 0 2 2.1 CN1CCN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2C1 10.1021/jm0612968
162647275 179538 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
CHEMBL4741776 179538 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1ccc(CCCc2cc(=O)c3c(O)cccc3o2)cc1 10.1016/j.bmcl.2020.127511
10150393 71880 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 373 7 0 4 3.2 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN(C)C 10.1016/j.bmcl.2005.08.004
CHEMBL197170 71880 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 373 7 0 4 3.2 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN(C)C 10.1016/j.bmcl.2005.08.004
10479309 79718 0 None -79 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 458 8 0 5 4.7 COc1ccc(N2CCC(c3ccc(OC)c(OCCN4CCCCC4)c3)C2=O)cc1Cl 10.1016/j.bmcl.2006.05.034
CHEMBL211719 79718 0 None -79 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 458 8 0 5 4.7 COc1ccc(N2CCC(c3ccc(OC)c(OCCN4CCCCC4)c3)C2=O)cc1Cl 10.1016/j.bmcl.2006.05.034
44414217 80114 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 516 7 0 4 6.3 O=C1C(c2ccc(Cl)c(Cl)c2)CCN1c1ccc(OC(F)(F)F)c(OCCN2CCCCC2)c1 10.1016/j.bmcl.2006.05.034
CHEMBL213368 80114 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 516 7 0 4 6.3 O=C1C(c2ccc(Cl)c(Cl)c2)CCN1c1ccc(OC(F)(F)F)c(OCCN2CCCCC2)c1 10.1016/j.bmcl.2006.05.034
24887284 141721 0 None -125 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL385921 141721 0 None -125 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
24888183 141794 0 None -1000 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 420 7 0 4 4.5 COc1ccc(N2CC=C(c3ccc(C)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL386332 141794 0 None -1000 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 420 7 0 4 4.5 COc1ccc(N2CC=C(c3ccc(C)cc3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
10296414 3505 15 None -1258 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
76 3505 15 None -1258 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
CHEMBL183460 3505 15 None -1258 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
11248705 90266 0 None -630 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238519 90266 0 None -630 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
91826739 121987 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 4 1 4 3.2 O=c1cc(COCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593952 121987 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 282 4 1 4 3.2 O=c1cc(COCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
168271856 190537 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5180016 190537 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
44572166 12428 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL1186133 12428 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
CHEMBL451232 12428 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 199 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccc(F)cc1Cl 10.1021/jm801354e
44572751 12467 1 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL1186509 12467 1 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
CHEMBL467736 12467 1 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NC[C@H]1C[C@@H]1c1ccccc1Br 10.1021/jm801354e
127026052 137528 0 None 4 19 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137528 0 None 4 19 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
145989551 167114 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 297 3 0 2 4.1 CN(C)CC/C=C1\c2ccc(F)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
CHEMBL4290607 167114 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 297 3 0 2 4.1 CN(C)CC/C=C1\c2ccc(F)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
70687202 77949 0 None -10 3 Human 6.8 pKi = 6.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
CHEMBL2096809 77949 0 None -10 3 Human 6.8 pKi = 6.8 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
11231392 84865 0 None -13 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223628 84865 0 None -13 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.6 CC(C)Oc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
11080 29054 79 None -6 6 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29054 79 None -6 6 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
59652086 114566 0 None -85 2 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2B
ChEMBL 448 8 2 6 3.6 COc1cccc(CNC(=O)c2nc3scc(CN(C)Cc4ccccc4)c3c(=O)[nH]2)c1 10.6019/CHEMBL5212743
CHEMBL3337895 114566 0 None -85 2 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HTR2B
ChEMBL 448 8 2 6 3.6 COc1cccc(CNC(=O)c2nc3scc(CN(C)Cc4ccccc4)c3c(=O)[nH]2)c1 10.6019/CHEMBL5212743
49865833 16132 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.2 O=C(Nc1ccccc1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224036 16132 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.2 O=C(Nc1ccccc1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
14702424 18532 69 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 176 2 2 2 1.6 COc1ccc2[nH]cc(CN)c2c1 10.1021/jm100600y
CHEMBL1276050 18532 69 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 176 2 2 2 1.6 COc1ccc2[nH]cc(CN)c2c1 10.1021/jm100600y
71462776 82934 0 None -134 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181169 82934 0 None -134 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
136118659 76226 0 None 1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058427 76226 0 None 1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
21527771 70127 1 None -645 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 70127 1 None -645 10 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
134135745 144354 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3905850 144354 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
134156506 154039 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3984645 154039 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 407 6 4 8 1.6 CC(C)[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
58911666 91062 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397886 91062 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
25120700 81210 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 369 7 1 5 3.0 COc1ccc(N2CCN(CC[C@@H](OC(N)=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.023
CHEMBL2158704 81210 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 369 7 1 5 3.0 COc1ccc(N2CCN(CC[C@@H](OC(N)=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.023
45486820 196911 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 432 3 2 4 3.8 O=c1[nH]c2cccc(N3C[C@H]4C[C@@H]3CN4CC3CCc4[nH]c5ccc(F)cc5c4C3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL1237149 196911 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 432 3 2 4 3.8 O=c1[nH]c2cccc(N3C[C@H]4C[C@@H]3CN4CC3CCc4[nH]c5ccc(F)cc5c4C3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL566356 196911 0 None -12 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 432 3 2 4 3.8 O=c1[nH]c2cccc(N3C[C@H]4C[C@@H]3CN4CC3CCc4[nH]c5ccc(F)cc5c4C3)c2o1 10.1016/j.bmcl.2009.08.050
45279963 80880 55 None 20 2 Human 6.8 pKi = 6.8 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 10.6019/CHEMBL4507316
CHEMBL2152944 80880 55 None 20 2 Human 6.8 pKi = 6.8 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 10.6019/CHEMBL4507316
71062768 143711 0 None -4 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL3900699 143711 0 None -4 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
3151 1450 97 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1450 97 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1450 97 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1450 97 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1450 97 None -125 27 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
44409317 141333 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@@H]2Cc3ccc(Br)nc3N21 10.1016/j.bmcl.2005.11.083
CHEMBL383694 141333 0 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@@H]2Cc3ccc(Br)nc3N21 10.1016/j.bmcl.2005.11.083
46884102 8030 1 None -912 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
CHEMBL1091106 8030 1 None -912 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
135501716 76284 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
CHEMBL2058695 76284 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
49783419 17717 0 None -501 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 17717 0 None -501 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
118055288 177012 0 None -58 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 2 3.0 CC1CN2CCNCc3cc(Cl)c(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4632473 177012 0 None -58 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 2 3.0 CC1CN2CCNCc3cc(Cl)c(Cl)c1c32 10.1016/j.bmcl.2019.126929
25209356 179761 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 544 7 2 8 4.0 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)c(Cl)c4=O)c3C)cc2)cn1 10.1021/jm800962k
CHEMBL474473 179761 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 544 7 2 8 4.0 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)c(Cl)c4=O)c3C)cc2)cn1 10.1021/jm800962k
127051015 140849 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140849 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140849 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
24826957 91088 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397912 91088 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
127049983 140637 1 None 7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(Cl)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814821 140637 1 None 7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(Cl)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127037093 136483 0 None 40 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736252 136483 0 None 40 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 433 11 0 5 4.8 COc1ccc(CCN(CCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
44435193 91196 0 None 1 7 Human 6.8 pKi = 6.8 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
CHEMBL240045 91196 0 None 1 7 Human 6.8 pKi = 6.8 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
CHEMBL5083607 214850 0 None -14 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL5093342 215541 0 None -19 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 215541 0 None -19 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
10334023 112855 5 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2BR (unknown origin) assessed as inhibition constant
ChEMBL 283 1 2 1 4.9 c1ccc2c(-c3nccc4c3[nH]c3ccccc34)c[nH]c2c1 10.1021/acs.jmedchem.0c01887
CHEMBL3309924 112855 5 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2BR (unknown origin) assessed as inhibition constant
ChEMBL 283 1 2 1 4.9 c1ccc2c(-c3nccc4c3[nH]c3ccccc34)c[nH]c2c1 10.1021/acs.jmedchem.0c01887
CHEMBL5268604 193550 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT2BR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2BR (unknown origin) assessed as inhibition constant
ChEMBL 299 1 3 2 4.6 Oc1ccc2[nH]c3c(-c4c[nH]c5ccccc45)nccc3c2c1 10.1021/acs.jmedchem.0c01887
162647063 179624 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 499 6 4 8 1.6 CC(C)[C@@H](Nc1nc(I)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
CHEMBL4743059 179624 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 499 6 4 8 1.6 CC(C)[C@@H](Nc1nc(I)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
162646751 179718 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 419 7 4 9 1.7 CSc1nc(N[C@H](C(C)C)C2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@]4(CO)C[C@H]34)c2n1 10.1016/j.bmcl.2020.127599
CHEMBL4744176 179718 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 419 7 4 9 1.7 CSc1nc(N[C@H](C(C)C)C2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@]4(CO)C[C@H]34)c2n1 10.1016/j.bmcl.2020.127599
90469115 185818 4 None -56 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185818 4 None -56 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
67978437 120651 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402657 120651 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547010 120651 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
44404887 134404 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 340 8 2 4 3.0 CCCCn1cc(CCN(C)C)c2c(OP(=O)(O)O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL371753 134404 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 340 8 2 4 3.0 CCCCn1cc(CCN(C)C)c2c(OP(=O)(O)O)cccc21 10.1016/j.bmcl.2005.06.104
127051015 140849 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140849 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140849 0 None -63 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11652359 89099 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1N(C)C2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337502 89099 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1N(C)C2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365706 89099 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1N(C)C2=O 10.1016/j.bmcl.2012.10.091
45279963 80880 55 None 20 2 Human 6.8 pKi = 6.8 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 10.6019/CHEMBL4507316
CHEMBL2152944 80880 55 None 20 2 Human 6.8 pKi = 6.8 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 10.6019/CHEMBL4507316
45279963 80880 55 None 20 2 Human 6.8 pKi = 6.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 10.6019/CHEMBL5212743
CHEMBL2152944 80880 55 None 20 2 Human 6.8 pKi = 6.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000717a HTR2B
ChEMBL 425 6 3 5 3.8 O=C1c2ccc(Nc3ccc(F)cc3F)cc2CCc2ccc(OC[C@H](O)CO)cc21 10.6019/CHEMBL5212743
46884101 8028 0 None -87 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 310 6 2 3 2.6 O=C(NCc1ccc(OCc2ccccc2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1091104 8028 0 None -87 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 310 6 2 3 2.6 O=C(NCc1ccc(OCc2ccccc2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
25263302 191960 0 None -134 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 191960 0 None -134 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2b receptorBinding affinity to 5HT2b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
44409290 74622 0 None -45 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203013 74622 0 None -45 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.7 C[C@@H]1CNC[C@H]2Cc3ccc(COCC4CC4)nc3N12 10.1016/j.bmcl.2005.11.083
16117279 60106 0 None -1778 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 60106 0 None -1778 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 60106 0 None -1778 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
57799326 89079 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337104 89079 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365468 89079 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 242 1 2 2 1.7 Cc1cc(C2CC2)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
145988693 167142 0 None -7 17 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 167142 0 None -7 17 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
153287572 173398 0 None 11 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 205 1 1 2 2.6 CC[C@H]1c2cc(C)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4528651 173398 0 None 11 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 205 1 1 2 2.6 CC[C@H]1c2cc(C)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
49865887 16149 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 302 1 1 3 3.0 O=C(NC1CCCCC1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224103 16149 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 302 1 1 3 3.0 O=C(NC1CCCCC1)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
1227 2472 43 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 2472 43 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 2472 43 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 2472 43 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 2472 43 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 2472 43 None -112 12 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
118055202 177170 0 None -12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.5 CC1(C)CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4635105 177170 0 None -12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 236 0 1 2 2.5 CC1(C)CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
118055282 177990 0 None -22 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 334 1 1 2 3.4 FC(F)(F)CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4646572 177990 0 None -22 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 334 1 1 2 3.4 FC(F)(F)CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
157 2056 7 None -20 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
9840090 2056 7 None -20 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
CHEMBL134519 2056 7 None -20 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm050663x
46230049 201522 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL605402 201522 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
18715564 73351 0 None -7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201454 73351 0 None -7 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 259 2 1 3 3.2 C[C@H](N)Cn1ccc2cc(Cl)c3ncccc3c21 10.1016/j.bmcl.2005.10.029
127053028 140617 1 None 8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(I)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814559 140617 1 None 8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2cccc(I)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127049982 140641 1 None 9 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2cccc(F)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3815000 140641 1 None 9 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 465 12 0 5 5.3 COc1ccc(CCN(CCCc2cccc(F)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
16115517 84809 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL223468 84809 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1ccc2c(c1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
23151712 120510 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 266 1 3 2 1.1 NC(N)=NC(=O)c1ccc2c(c1)C(N)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310120 120510 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 266 1 3 2 1.1 NC(N)=NC(=O)c1ccc2c(c1)C(N)c1ccccc1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545471 120510 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 266 1 3 2 1.1 NC(N)=NC(=O)c1ccc2c(c1)C(N)c1ccccc1-2 10.1016/j.bmc.2014.05.027
157 2056 7 None -20 4 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm030205t
9840090 2056 7 None -20 4 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm030205t
CHEMBL134519 2056 7 None -20 4 Human 7.8 pKi = 7.8 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/jm030205t
49862237 14975 0 None -11 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 395 6 0 5 4.3 COc1ccc(OC)c(C2CCN(Cc3cnn(-c4ccccc4F)c3C)C2)c1 10.1016/j.bmcl.2010.06.033
CHEMBL1209157 14975 0 None -11 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 395 6 0 5 4.3 COc1ccc(OC)c(C2CCN(Cc3cnn(-c4ccccc4F)c3C)C2)c1 10.1016/j.bmcl.2010.06.033
1524 2168 96 None -229 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
197 2168 96 None -229 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
3822 2168 96 None -229 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
88 2168 96 None -229 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
CHEMBL51 2168 96 None -229 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
DB12465 2168 96 None -229 52 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 minsDisplacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.bmcl.2013.01.025
118055199 177931 0 None -33 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 1.9 CC1(C)CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
CHEMBL4645774 177931 0 None -33 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 1.9 CC1(C)CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
44409124 74440 0 None -30 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 214 0 1 4 0.7 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL202795 74440 0 None -30 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 214 0 1 4 0.7 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)nc3N12 10.1016/j.bmcl.2005.11.083
46914777 15411 0 None 18 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1215038 15411 0 None 18 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
33630 178933 99 None -6 28 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178933 99 None -6 28 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
44582677 181549 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 432 10 1 6 3.9 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476838 181549 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 432 10 1 6 3.9 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.bmc.2009.03.021
71061729 160919 0 None -1 4 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4115493 160919 0 None -1 4 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
25117679 200581 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599263 200581 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
142601318 185521 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863036 185521 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
134138183 147786 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3932820 147786 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
155567457 175925 0 None -158 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 359 2 3 6 2.8 O[C@H]1CCC[C@@H]1Nc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
CHEMBL4587951 175925 0 None -158 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cell by radioligand binding assay
ChEMBL 359 2 3 6 2.8 O[C@H]1CCC[C@@H]1Nc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
46914926 15399 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214960 15399 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
11579853 89056 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337504 89056 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365200 89056 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
119584 2577 102 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
1848 2577 102 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
242 2577 102 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL60889 2577 102 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
DB11675 2577 102 None 1 6 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl nan
CHEMBL4750687 214014 0 None - 1 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000312b HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000312b HTR2B
ChEMBL None None None Cc1ncc(-c2cc(Cl)ccc2F)cc1-n1c(=O)n(CC(N)=O)c2cnccc21 10.6019/CHEMBL5212743
CHEMBL4741904 214009 0 None - 1 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000710a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000710a HTR2B
ChEMBL None None None Cc1ncc(-c2cc(Cl)ccc2F)cc1-n1c(=O)n(CC(N)=O)c2ccccc21 10.6019/CHEMBL5212743
44316027 205499 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL80862 205499 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 236 4 1 3 2.5 CCSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
11658860 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
2941 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
4374 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
CHEMBL360328 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
DB04871 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1021/jm801354e
CHEMBL5074880 214316 0 None -1 9 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
9899500 67860 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
CHEMBL191054 67860 0 None -14 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
11391654 180501 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4753511 180501 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
24873384 182577 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 255 2 1 3 2.8 CC(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4788223 182577 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 255 2 1 3 2.8 CC(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
134154065 152337 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3970041 152337 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 433 6 3 9 1.5 COC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
11020695 25482 1 None -5 3 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL135076 25482 1 None -5 3 Human 7.7 pKi = 7.7 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
879244 28168 8 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
CHEMBL1373650 28168 8 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 271 1 3 5 2.3 Cc1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acsmedchemlett.8b00300
10791286 35287 0 None -9 2 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 491 3 1 3 6.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(Br)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14368 35287 0 None -9 2 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 491 3 1 3 6.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(Br)cc(-c3cccnc3)c1)CC2 10.1021/jm990388c
10526616 39476 0 None -15 3 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 430 4 1 5 4.9 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3)nc1)CC2 10.1021/jm990388c
CHEMBL14726 39476 0 None -15 3 Human 7.7 pKi = 7.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 430 4 1 5 4.9 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3)nc1)CC2 10.1021/jm990388c
44298229 101897 0 None -31 3 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL301012 101897 0 None -31 3 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
147653864 171537 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 0 1 2 2.7 C[C@@]12COc3c(Br)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4464697 171537 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 267 0 1 2 2.7 C[C@@]12COc3c(Br)cccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
153061504 172786 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4513930 172786 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
2389 3306 118 None -66 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073 3306 118 None -66 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
96 3306 118 None -66 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
CHEMBL85 3306 118 None -66 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
DB00734 3306 118 None -66 68 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
2267 557 71 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
271 557 71 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
7121 557 71 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
CHEMBL639 557 71 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
DB00972 557 71 None -10 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
44298118 193387 0 None -1 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 5 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL52592 193387 0 None -1 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 5 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
12017599 195761 0 None -6 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 426 4 1 3 5.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(CCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55784 195761 0 None -6 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 426 4 1 3 5.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(CCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
72698088 103962 0 None -954 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093187 103962 0 None -954 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 421 6 0 4 5.4 Fc1cccc2c1nc(OCC1CCN(CCCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
11175045 136516 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.9 CC(C)c1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL373695 136516 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.9 CC(C)c1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
135474338 189247 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL511879 189247 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
54761054 138056 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Positive allosteric modulation of 5-HT2B receptor (unknown origin)Positive allosteric modulation of 5-HT2B receptor (unknown origin)
ChEMBL 367 3 1 5 4.0 Cc1ccc(C(C)(C)O)cc1-c1ccc2c(n1)n(C)c(=O)n2CC(C)(C)C 10.1016/j.bmcl.2016.01.021
CHEMBL3765778 138056 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Positive allosteric modulation of 5-HT2B receptor (unknown origin)Positive allosteric modulation of 5-HT2B receptor (unknown origin)
ChEMBL 367 3 1 5 4.0 Cc1ccc(C(C)(C)O)cc1-c1ccc2c(n1)n(C)c(=O)n2CC(C)(C)C 10.1016/j.bmcl.2016.01.021
134149168 148222 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
CHEMBL3936289 148222 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
11499800 89078 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337503 89078 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365465 89078 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 216 0 2 2 1.1 Cc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
25117680 200612 0 None -13 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599466 200612 0 None -13 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
155536619 172177 0 None -75 4 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 254 3 4 7 -2.3 NC(=O)c1ncn([C@H]2[C@H](O)[C@H](O)[C@]3(CO)C[C@H]23)n1 10.1021/acs.jmedchem.8b01662
CHEMBL4473739 172177 0 None -75 4 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 254 3 4 7 -2.3 NC(=O)c1ncn([C@H]2[C@H](O)[C@H](O)[C@]3(CO)C[C@H]23)n1 10.1021/acs.jmedchem.8b01662
122178710 121350 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OCc1ccccc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581255 121350 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OCc1ccccc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
11290492 137976 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL376456 137976 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 218 1 1 3 0.8 COc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
5318 15544 49 None -1 13 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15544 49 None -1 13 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15544 49 None -1 13 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
1531 2253 69 None -16 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2253 69 None -16 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2253 69 None -16 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2253 69 None -16 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2253 69 None -16 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
124 2960 47 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2960 47 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2960 47 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2960 47 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2960 47 None -181 33 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
11416698 91078 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397902 91078 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
73349359 92514 0 None -2 8 Human 5.7 pKi = 5.7 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432051 92514 0 None -2 8 Human 5.7 pKi = 5.7 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
44582708 186814 0 None -1 5 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 415 10 0 5 4.2 COc1ccc(CCN2CCC(C(=O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
CHEMBL489408 186814 0 None -1 5 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 415 10 0 5 4.2 COc1ccc(CCN2CCC(C(=O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
3191 102831 97 None -7 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102831 97 None -7 25 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
44414251 78044 0 None -158 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 470 7 0 4 4.8 COc1ccc(N2CC=C(c3ccc(Br)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL210053 78044 0 None -158 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 470 7 0 4 4.8 COc1ccc(N2CC=C(c3ccc(Br)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
44414070 79891 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 474 7 0 4 5.7 COc1ccc(C2=C(C)CN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL212482 79891 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 474 7 0 4 5.7 COc1ccc(C2=C(C)CN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
49850672 56356 0 None -794 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 404 5 1 5 4.1 COC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1631532 56356 0 None -794 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 404 5 1 5 4.1 COC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
44298021 194736 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 4 1 4 5.9 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C(C)C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL53793 194736 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 422 4 1 4 5.9 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3C(C)C)nc1)CC2 10.1016/s0960-894x(00)00364-4
18931377 206452 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/S0960-894X(96)00503-3
CHEMBL88193 206452 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/S0960-894X(96)00503-3
18931150 206805 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1cc(Cl)ccc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL90470 206805 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1cc(Cl)ccc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
153287566 171156 0 None -74 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 278 1 0 2 4.0 CN1CC[C@H]2c3ccccc3N(c3ccccc3)C[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4459009 171156 0 None -74 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 278 1 0 2 4.0 CN1CC[C@H]2c3ccccc3N(c3ccccc3)C[C@]21C 10.1021/acsmedchemlett.9b00225
11292350 87912 0 None -79 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 394 6 0 4 4.3 COc1ccc(N2Cc3cccc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234006 87912 0 None -79 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 394 6 0 4 4.3 COc1ccc(N2Cc3cccc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11775262 88026 0 None -125 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234532 88026 0 None -125 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11430311 150023 0 None -158 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 428 6 0 4 5.2 COc1ccc(N2C(=O)c3c(Cl)cccc3C2C)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL395059 150023 0 None -158 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 428 6 0 4 5.2 COc1ccc(N2C(=O)c3c(Cl)cccc3C2C)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11453704 150042 0 None -79 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.4 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCCCC1 10.1016/j.bmcl.2006.10.029
CHEMBL395072 150042 0 None -79 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.4 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCCCCC1 10.1016/j.bmcl.2006.10.029
11282335 150299 0 None -39 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)c(Cl)cc3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL395297 150299 0 None -39 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.3 COc1ccc(N2Cc3cc(Cl)c(Cl)cc3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
11753782 12774 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 4.2 COc1ccc(N2Cc3c(c4ccccc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL1188213 12774 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 4.2 COc1ccc(N2Cc3c(c4ccccc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL535626 12774 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 4.2 COc1ccc(N2Cc3c(c4ccccc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
10458785 86733 0 None -50 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232045 86733 0 None -50 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4ccc(Cl)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
10346749 88378 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 487 6 0 5 5.5 COc1ccc(N2Cc3c(c4cc(Cl)c(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
CHEMBL234947 88378 0 None -31 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 487 6 0 5 5.5 COc1ccc(N2Cc3c(c4cc(Cl)c(Cl)cc4n3C)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.034
10390089 142336 0 None -125 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 436 6 0 5 5.2 COc1ccc(N2Cc3sc4ccccc4c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL388882 142336 0 None -125 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 436 6 0 5 5.2 COc1ccc(N2Cc3sc4ccccc4c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
44298138 195478 0 None -39 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(COc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55344 195478 0 None -39 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(COc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
162660908 181396 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4763861 181396 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 294 4 1 3 4.0 Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
162669225 182740 0 None - 1 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2cccc(Cl)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4790230 182740 0 None - 1 Human 5.7 pKi = 5.7 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2cccc(Cl)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
10812577 99017 1 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3cccnc3)ccc1F)CC2 10.1021/jm990388c
CHEMBL280322 99017 1 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(-c3cccnc3)ccc1F)CC2 10.1021/jm990388c
10249573 207570 0 None -199 11 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL94984 207570 0 None -199 11 Human 5.7 pKi = 5.7 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
10237852 72375 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 411 7 0 6 3.6 COc1ccc(-n2ccn(-c3cccc(F)c3)c2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198712 72375 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 411 7 0 6 3.6 COc1ccc(-n2ccn(-c3cccc(F)c3)c2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
24887517 169015 0 None -158 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL439504 169015 0 None -158 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 476 7 0 4 5.6 COc1ccc(N2CCC(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
11191906 11735 0 None -39 12 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 11735 0 None -39 12 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 11735 0 None -39 12 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 2B expressed in HEK 293 cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
44298079 196300 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 346 3 1 4 4.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL56232 196300 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 346 3 1 4 4.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccccc32)cn1 10.1016/s0960-894x(00)00364-4
44298193 199355 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL59097 199355 0 None -316 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)ccc32)cn1 10.1016/s0960-894x(00)00364-4
10433930 51059 0 None -999 5 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157910 51059 0 None -999 5 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
118278424 121986 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 256 3 1 4 2.9 O=c1cc(CCc2ccco2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3593951 121986 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 256 3 1 4 2.9 O=c1cc(CCc2ccco2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
24865725 188060 0 None -3981 12 Human 5.7 pKi = 5.7 Binding
Displacement of radioligand from human cloned 5HT2B receptorDisplacement of radioligand from human cloned 5HT2B receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL497963 188060 0 None -3981 12 Human 5.7 pKi = 5.7 Binding
Displacement of radioligand from human cloned 5HT2B receptorDisplacement of radioligand from human cloned 5HT2B receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
9892409 100923 0 None -398 9 Human 5.7 pKi = 5.7 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29410 100923 0 None -398 9 Human 5.7 pKi = 5.7 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
448537 160226 89 None -21 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160226 89 None -21 25 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
11957541 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
1229 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
147 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
170617 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
CHEMBL6616 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5-HT2B receptor by radioligand displacement assayBinding affinity to human 5-HT2B receptor by radioligand displacement assay
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1016/j.ejmech.2013.01.044
11957541 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
1229 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
147 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
170617 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
CHEMBL6616 1446 40 None -2 16 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)-DOI from human 5HT2B receptorDisplacement of [125I](+/-)-DOI from human 5HT2B receptor
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm2006782
24826867 91066 0 None 3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397890 91066 0 None 3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
11323169 179943 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 2 1 3 3.1 Cc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4746737 179943 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 2 1 3 3.1 Cc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
2220 3112 82 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
27400 3112 82 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
93 3112 82 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
CHEMBL294951 3112 82 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
DB06153 3112 82 None -1 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1016/j.bmc.2013.10.010
118717217 120550 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343667 120550 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545762 120550 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 325 4 2 3 1.6 COCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
72734862 106279 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 253 1 2 2 2.0 NC(N)=NC(=O)c1ccc2c(c1)oc1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3092754 106279 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 253 1 2 2 2.0 NC(N)=NC(=O)c1ccc2c(c1)oc1ccccc12 10.1016/j.bmc.2013.10.010
CHEMBL3139079 106279 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 253 1 2 2 2.0 NC(N)=NC(=O)c1ccc2c(c1)oc1ccccc12 10.1016/j.bmc.2013.10.010
44269058 31336 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL14022 31336 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/ml3003814
157 2056 7 None -20 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/acs.jmedchem.1c00726
9840090 2056 7 None -20 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/acs.jmedchem.1c00726
CHEMBL134519 2056 7 None -20 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 10.1021/acs.jmedchem.1c00726
1043 1569 14 None -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1569 14 None -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1569 14 None -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1569 14 None -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1569 14 None -22 29 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
10251906 67754 18 None -186 7 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysisBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysis
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1021/acs.jmedchem.2c00633
CHEMBL1908863 67754 18 None -186 7 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysisBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysis
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1021/acs.jmedchem.2c00633
CHEMBL482496 67754 18 None -186 7 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysisBinding affinity to 5-HT2B (unknown origin) assessed as inhibition constant by liquid scintillation counter analysis
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1021/acs.jmedchem.2c00633
72734867 106339 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Oc1ccccc1N2 10.1016/j.bmc.2013.10.010
CHEMBL3092757 106339 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Oc1ccccc1N2 10.1016/j.bmc.2013.10.010
CHEMBL3139241 106339 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Oc1ccccc1N2 10.1016/j.bmc.2013.10.010
230 4088 25 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.12.009
3045225 4088 25 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.12.009
CHEMBL407909 4088 25 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 243 3 1 4 2.7 CCc1oc2c(c1)c1c(cc2)cnn1C[C@@H](N)C 10.1016/j.bmc.2007.12.009
67781610 166930 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 0 2 4.7 CN(C)CC/C=C1\c2ccc(Br)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
CHEMBL4287193 166930 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 0 2 4.7 CN(C)CC/C=C1\c2ccc(Br)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
16062910 97399 0 None -6 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 329 3 1 3 3.7 Cc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL269974 97399 0 None -6 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 329 3 1 3 3.7 Cc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
9839920 101681 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 316 2 2 3 4.4 Cn1ccc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
CHEMBL299498 101681 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 316 2 2 3 4.4 Cn1ccc2cc(NC(=O)Nc3ccnc4ccccc34)ccc21 10.1016/s0960-894x(01)00343-2
146709966 175755 0 None 338 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4583909 175755 0 None 338 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
1042 1568 23 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1568 23 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1568 23 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1568 23 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1568 23 None -7 17 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
11536844 115096 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343672 115096 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
206 2476 16 None -1 25 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
68848 2476 16 None -1 25 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL12314 2476 16 None -1 25 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1016/j.ejmech.2019.04.064
4376990 192985 5 None -1 11 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192985 5 None -1 11 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192985 5 None -1 11 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
153061504 172786 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4513930 172786 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2c(ccc3ccccc23)OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
59752538 181128 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 339 3 1 4 3.7 CC(C)n1nc2c(c1-c1ccc(OC(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4760784 181128 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 339 3 1 4 3.7 CC(C)n1nc2c(c1-c1ccc(OC(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
11414582 181314 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 271 2 1 3 2.7 Fc1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4762886 181314 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 271 2 1 3 2.7 Fc1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
59752638 182373 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 253 2 1 3 2.6 c1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4785470 182373 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 253 2 1 3 2.6 c1ccc(-c2c3c(nn2C2CC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
189 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jnatprod.2c00365
5163 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jnatprod.2c00365
CHEMBL297784 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/acs.jnatprod.2c00365
3037629 184548 18 None 1 10 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4848517 184548 18 None 1 10 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
66647021 120650 0 None -9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402656 120650 0 None -9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547009 120650 0 None -9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 257 2 0 1 4.2 CN(C)[C@@H]1Cc2ccccc2[C@@H](C2CCCCC2)C1 10.1016/j.bmc.2015.01.060
118729256 120683 0 None 6 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402670 120683 0 None 6 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547156 120683 0 None 6 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
16062785 95092 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 2 1 3 3.1 CC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL255543 95092 0 None -5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 2 1 3 3.1 CC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
16062784 95138 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 318 2 1 4 3.4 N#Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL255802 95138 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 318 2 1 4 3.4 N#Cc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
752521 198714 8 None 12 9 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 198714 8 None 12 9 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
118729260 120662 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402672 120662 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547044 120662 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
118729274 120685 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402681 120685 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547175 120685 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
44435219 91763 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL241115 91763 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
155556618 174453 0 None -1905 5 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 417 6 3 7 2.7 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)ncnc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4554295 174453 0 None -1905 5 Human 5.7 pKi = 5.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 417 6 3 7 2.7 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)ncnc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
5897 105184 80 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
CHEMBL311469 105184 80 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 223 1 1 1 3.2 CC(=O)Nc1ccc2c(c1)Cc1ccccc1-2 nan
9926401 140850 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140850 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140850 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
71459553 83667 10 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 406 7 0 4 5.3 COc1ccc2c(C)c(C(=O)N(CCCN3CCCCC3)c3ccccc3)oc2c1 10.1016/j.bmc.2012.09.044
CHEMBL2205360 83667 10 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 406 7 0 4 5.3 COc1ccc2c(C)c(C(=O)N(CCCN3CCCCC3)c3ccccc3)oc2c1 10.1016/j.bmc.2012.09.044
9926401 140850 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140850 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140850 0 None -4 8 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
155554410 174370 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 331 2 2 5 0.6 Cc1cccc(C)c1N1C(=O)[C@H](CO)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4552298 174370 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 331 2 2 5 0.6 Cc1cccc(C)c1N1C(=O)[C@H](CO)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
11615459 199225 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590078 199225 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
122186881 122955 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608451 122955 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
11209786 137215 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375170 137215 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 296 1 1 2 2.7 O=C1c2c(cc(C3CC3)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
155558626 174737 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4561016 174737 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
11336079 83447 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 280 0 1 2 1.8 C#Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL220115 83447 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 280 0 1 2 1.8 C#Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
11264955 204938 0 None -6 3 Human 7.7 pKi = 7.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL76474 204938 0 None -6 3 Human 7.7 pKi = 7.7 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 240 3 1 3 2.3 CSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
20824945 67558 0 None -16 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL190124 67558 0 None -16 3 Human 7.7 pKi = 7.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
196129 67769 17 None -26 15 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67769 17 None -26 15 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
118055334 177446 0 None -34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 266 0 1 2 2.5 CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4639090 177446 0 None -34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 266 0 1 2 2.5 CC1CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
24826963 91086 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397910 91086 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
71681897 91090 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
CHEMBL2397914 91090 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
25123014 200408 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598229 200408 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
126769 206019 42 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1016/j.bmcl.2016.05.079
CHEMBL536255 206019 42 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1016/j.bmcl.2016.05.079
CHEMBL85194 206019 42 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 2 3 3.2 Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc21 10.1016/j.bmcl.2016.05.079
189 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C4MD00418C
5163 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C4MD00418C
CHEMBL297784 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C4MD00418C
127037059 136512 0 None 10 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3736516 136512 0 None 10 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 445 11 0 5 5.6 COc1ccc(CCN(CC/C=C\c2ccccc2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL4777443 214023 0 None 11 14 Human 7.7 pKi = 7.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR2B
ChEMBL None None None CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1 10.6019/CHEMBL5212743
70687202 77949 0 None -10 3 Human 6.7 pKi = 6.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
CHEMBL2096809 77949 0 None -10 3 Human 6.7 pKi = 6.7 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@@H]1CNC[C@@H]2Cc3ccccc3N21 10.1016/j.bmcl.2005.05.074
18715558 73853 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL201897 73853 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3ccncc3c21 10.1016/j.bmcl.2005.10.029
44451390 155726 2 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 210 1 2 2 2.1 CNc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL405717 155726 2 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 210 1 2 2 2.1 CNc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
118729246 120661 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402663 120661 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547043 120661 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
16062143 97666 0 None -19 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 283 2 1 3 3.2 Fc1ccc(-c2nc(C3CCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271318 97666 0 None -19 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 283 2 1 3 3.2 Fc1ccc(-c2nc(C3CCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
134146585 148885 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 366 3 3 8 -0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3941738 148885 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 366 3 3 8 -0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
117209911 186305 1 None -26 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4874854 186305 1 None -26 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
24826786 91057 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397881 91057 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
10330266 21371 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2ccsc12 10.1021/jm980692q
CHEMBL13147 21371 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from cloned human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2ccsc12 10.1021/jm980692q
4011 82379 49 None -20 24 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82379 49 None -20 24 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
155512086 169597 0 None -407 5 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 399 6 4 8 1.5 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4436786 169597 0 None -407 5 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 399 6 4 8 1.5 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
137645406 157878 0 None -269 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4084262 157878 0 None -269 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4526351 213960 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000703a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000703a HTR2B
ChEMBL None None None Cc1cc(NC(=O)c2cccc(S(F)(F)(F)(F)F)c2)cc(-n2ccn3nc(-c4cccnc4)cc23)c1 10.6019/CHEMBL5212743
117209857 185114 1 None -5 8 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 185114 1 None -5 8 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
4601 206724 35 None -4 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206724 35 None -4 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206724 35 None -4 17 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
68617 205504 62 None -15 26 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL1709 205504 62 None -15 26 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
CHEMBL809 205504 62 None -15 26 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 nan
104697662 145380 1 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
CHEMBL3914002 145380 1 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 293 3 2 4 3.3 Clc1cccc(CNc2nc(Cl)nc3[nH]cnc23)c1 10.1021/acs.jmedchem.6b01183
71682217 91089 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397913 91089 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 1 1 3 1.0 COc1c(C)ccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44409032 74993 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@@H]2Cc3ccc(Cl)nc3N21 10.1016/j.bmcl.2005.11.083
CHEMBL203396 74993 0 None -4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@@H]2Cc3ccc(Cl)nc3N21 10.1016/j.bmcl.2005.11.083
165193 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3165 68 None -72 43 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2353 101085 82 None -7 5 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL12089 101085 82 None -7 5 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
CHEMBL295124 101085 82 None -7 5 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 336 2 0 4 3.1 COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2 nan
10440 2662 20 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2662 20 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2662 20 None 3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
3117 207818 103 None -8 16 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207818 103 None -8 16 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
145992489 166953 0 None -6 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4287623 166953 0 None -6 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
118055195 177993 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 2.0 Cc1ccc2c3c1C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4646618 177993 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 202 0 1 2 2.0 Cc1ccc2c3c1C(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
122178704 121344 0 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581249 121344 0 None 1 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
16047544 12616 8 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187185 12616 8 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL492916 12616 8 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
16062911 97683 0 None -27 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 383 3 1 3 4.4 FC(F)(F)c1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271418 97683 0 None -27 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 383 3 1 3 4.4 FC(F)(F)c1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
189 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C8MD00204E
5163 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C8MD00204E
CHEMBL297784 3466 39 None -5 17 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1039/C8MD00204E
11658860 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
2941 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
4374 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
CHEMBL360328 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
DB04871 2329 51 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1016/j.bmcl.2019.126929
11187156 136329 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 312 3 1 2 3.1 CCCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL373483 136329 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 312 3 1 2 3.1 CCCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
16062270 97645 0 None -100 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 297 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271212 97645 0 None -100 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 297 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
16062266 97665 0 None -169 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 337 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271317 97665 0 None -169 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 337 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CNCC3)cc1 10.1016/j.bmcl.2008.01.090
2284 3160 33 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3160 33 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3160 33 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3160 33 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3160 33 None -16 29 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
9837204 74664 1 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 209 0 1 3 1.1 Clc1ccc2c(n1)N1CCNCC1C2 10.1016/j.bmcl.2005.11.083
CHEMBL203025 74664 1 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 209 0 1 3 1.1 Clc1ccc2c(n1)N1CCNCC1C2 10.1016/j.bmcl.2005.11.083
49865829 16127 0 None 22 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 330 1 1 3 4.1 O=C(Nc1ccccc1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224031 16127 0 None 22 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 330 1 1 3 4.1 O=C(Nc1ccccc1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
51352628 82798 10 None -1 3 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 353 5 0 7 2.1 COCCc1ccc(-c2c(C)nc3c(N4CCOCC4)ccnn23)cn1 10.6019/CHEMBL4800727
CHEMBL2180408 82798 10 None -1 3 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 353 5 0 7 2.1 COCCc1ccc(-c2c(C)nc3c(N4CCOCC4)ccnn23)cn1 10.6019/CHEMBL4800727
16062139 157643 0 None -204 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.4 CCC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL408154 157643 0 None -204 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.4 CCC(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
71463061 83766 0 None -3 9 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205813 83766 0 None -3 9 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
2351 3261 64 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3261 64 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3261 64 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3261 64 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3261 64 None -7 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
156012918 177424 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.2 Clc1ccc2c3c1CCCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4638807 177424 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.2 Clc1ccc2c3c1CCCN3CCNC2 10.1016/j.bmcl.2019.126929
24826870 91074 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397898 91074 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
444795 139974 105 None 3 2 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
CHEMBL38 139974 105 None 3 2 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 nan
136118613 93034 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442275 93034 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
51352628 82798 10 None -1 3 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 353 5 0 7 2.1 COCCc1ccc(-c2c(C)nc3c(N4CCOCC4)ccnn23)cn1 10.6019/CHEMBL4800727
CHEMBL2180408 82798 10 None -1 3 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 353 5 0 7 2.1 COCCc1ccc(-c2c(C)nc3c(N4CCOCC4)ccnn23)cn1 10.6019/CHEMBL4800727
CHEMBL5271021 193643 0 None 11 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1039/D1MD00167A
26987 946 33 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 946 33 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 946 33 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 946 33 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 946 33 None -47 21 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
46230099 199289 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590483 199289 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CCNCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
11514226 89081 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337494 89081 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365470 89081 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 202 0 2 2 0.8 Cc1cccc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
15560577 185317 9 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4859858 185317 9 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control
ChEMBL 398 5 1 5 3.8 CC[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
134152052 153059 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3976121 153059 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
134152052 153059 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL3976121 153059 0 None 3 5 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 432 6 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL5094493 215476 0 None -11 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
72698087 103961 0 None -2089 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
CHEMBL3093186 103961 0 None -2089 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2BBinding affinity to human 5HT2B
ChEMBL 407 5 0 4 5.0 Fc1cccc2c1nc(OCC1CCN(CCC(F)(F)F)CC1)c1cccnc12 10.1016/j.bmc.2013.08.061
10251906 67754 18 None -186 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
CHEMBL1908863 67754 18 None -186 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
CHEMBL482496 67754 18 None -186 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
155539605 172821 0 None 3 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4514672 172821 0 None 3 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
127034730 136414 0 None 9 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735643 136414 0 None 9 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 523 14 0 8 5.1 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
46914927 15387 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214893 15387 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 382 8 0 4 4.5 FCCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
91864602 140713 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140713 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
135514796 93029 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442270 93029 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
142601323 185817 0 None -9 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4867560 185817 0 None -9 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1ccccc1-c1n[nH]cc1N1CCCNCC1 10.1021/acs.jmedchem.1c01093
3973 208157 110 None -44 3 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
CHEMBL98350 208157 110 None -44 3 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 2 0 4 3.3 O=c1cc(N2CCOCC2)oc2c(-c3ccccc3)cccc12 nan
3157 1458 71 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1458 71 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1458 71 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1458 71 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1458 71 None -37 12 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
91864602 140713 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140713 0 None -66 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
16115388 137341 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL375302 137341 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 1 1 2 2.6 CC[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
11185858 84763 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL223271 84763 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
71061785 160472 0 None -6 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL4112056 160472 0 None -6 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10430623 18643 24 None -213 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1277105 18643 24 None -213 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
72901200 119751 25 None -162 4 Human 6.6 pKi = 6.6 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2BSelectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2B
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
CHEMBL3480577 119751 25 None -162 4 Human 6.6 pKi = 6.6 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2BSelectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HTR2B
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
11587397 89027 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337489 89027 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2364893 89027 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
6726 1269 51 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1269 51 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1269 51 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1269 51 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1269 51 None -7 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44579715 193228 0 None -2238 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 4 3 7 2.7 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Cl)c3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
CHEMBL523797 193228 0 None -2238 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 405 4 3 7 2.7 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Cl)c3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
46230048 199267 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590332 199267 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
118055215 177432 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 216 0 1 2 2.2 Cc1ccc2c3c1C(C)(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4638879 177432 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 216 0 1 2 2.2 Cc1ccc2c3c1C(C)(C)CN3CCNC2 10.1016/j.bmcl.2019.126929
1355 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
142 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
CHEMBL478 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
DB12110 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2009.12.014
11652452 89097 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337492 89097 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365703 89097 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 270 0 1 2 1.8 CN1C(=O)c2c(cccc2C(F)(F)F)[C@H]2CNC[C@@H]21 10.1016/j.bmcl.2012.10.091
162668650 182649 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 284 3 2 4 2.9 CNc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4789085 182649 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 284 3 2 4 2.9 CNc1ccc(-c2c3c(nn2C(C)C)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
3251 4041 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
5684 4041 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
80 4041 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
CHEMBL31354 4041 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
1355 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
142 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
CHEMBL478 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
DB12110 1998 88 None -1 16 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0612968
16115381 83414 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
CHEMBL219837 83414 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1NCCN2C(=O)c3c(cccc3C(F)(F)F)[C@H]12 10.1021/jm0612968
10015055 2090 4 None -120 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
1212 2090 4 None -120 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
CHEMBL3402679 2090 4 None -120 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
46884100 7985 0 None -104 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 314 5 2 3 3.0 O=C(NCc1ccc(Oc2cccc(F)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1090757 7985 0 None -104 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 314 5 2 3 3.0 O=C(NCc1ccc(Oc2cccc(F)c2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
145978665 163494 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 246 2 2 3 2.4 C[C@@H]1SC(c2c[nH]c3ccccc23)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4202582 163494 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 246 2 2 3 2.4 C[C@@H]1SC(c2c[nH]c3ccccc23)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
2142 3074 58 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
4920903 3074 58 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
502 3074 58 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
5775 3074 58 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
CHEMBL597 3074 58 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
DB00692 3074 58 None -43 37 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 nan
56678761 65638 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1cccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
CHEMBL1834257 65638 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1cccc(CCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
46914773 15397 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214958 15397 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
9921064 127152 25 None -8 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
CHEMBL365751 127152 25 None -8 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
22254068 65940 32 None -173 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836317 65940 32 None -173 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
11536299 183262 8 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
CHEMBL479683 183262 8 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 266 3 1 3 3.3 O=c1cc(CCc2ccccc2)oc2cccc(O)c12 10.1016/j.bmcl.2014.02.029
145990586 166819 0 None -19 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166819 0 None -19 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
136118660 76227 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058428 76227 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
135367816 164811 0 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164811 0 None -3 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
11483068 84783 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223440 84783 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
11414184 83469 0 None -13 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
CHEMBL220274 83469 0 None -13 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)C2CNCCN12 10.1021/jm0612968
43922 114739 10 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 250 4 2 2 2.0 COc1cc2c(CCNC(C)=O)c[nH]c2cc1F 10.1021/jm100600y
CHEMBL333886 114739 10 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 250 4 2 2 2.0 COc1cc2c(CCNC(C)=O)c[nH]c2cc1F 10.1021/jm100600y
1212 1649 50 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1649 50 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1649 50 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1649 50 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1649 50 None -27 66 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
9856509 95938 4 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 259 0 1 1 2.8 Clc1c(Br)ccc2c1CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL259480 95938 4 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 259 0 1 1 2.8 Clc1c(Br)ccc2c1CCNCC2 10.1016/j.bmc.2007.12.009
168293016 192086 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5203303 192086 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 7 0 5 5.0 CCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
10599545 36372 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Cl)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14469 36372 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Cl)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
10436045 3490 4 None -7 13 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3490 4 None -7 13 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3490 4 None -7 13 Human 7.6 pKi = 7.6 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
189 3466 39 None -5 17 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970741j
5163 3466 39 None -5 17 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970741j
CHEMBL297784 3466 39 None -5 17 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970741j
11391654 180501 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4753511 180501 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 273 2 1 3 3.0 CC(C)n1nc2c(c1-c1ccc(F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
189 3466 39 None -5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970424c
5163 3466 39 None -5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970424c
CHEMBL297784 3466 39 None -5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cellsDisplacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm970424c
10835537 38597 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccccc3)c1)CC2 10.1021/jm990388c
CHEMBL14652 38597 0 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccccc3)c1)CC2 10.1021/jm990388c
10574607 40614 0 None -7 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3ccncc3)c1)CC2 10.1021/jm990388c
CHEMBL14841 40614 0 None -7 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3ccncc3)c1)CC2 10.1021/jm990388c
44298249 194561 0 None 1 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3cccnc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL53063 194561 0 None 1 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3cccnc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
44298121 194805 0 None -3 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cccc(COc2ccc(NC(=O)N3CCc4cc(C)c(C(F)(F)F)cc43)cn2)n1 10.1016/s0960-894x(00)00365-6
CHEMBL53939 194805 0 None -3 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cccc(COc2ccc(NC(=O)N3CCc4cc(C)c(C(F)(F)F)cc43)cn2)n1 10.1016/s0960-894x(00)00365-6
44214723 195471 0 None -10 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 427 4 1 3 5.6 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)cc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55335 195471 0 None -10 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 427 4 1 3 5.6 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)cc1)CC2 10.1016/s0960-894x(00)00365-6
1225 1459 26 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
3958 1459 26 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
667477 1459 26 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
CHEMBL860 1459 26 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
DB01142 1459 26 None -89 22 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acsmedchemlett.8b00300
20824946 123617 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 218 1 2 3 0.9 C[C@@H]1CNC[C@H]2Cc3ccc(CO)cc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL361929 123617 0 None -7 3 Human 6.6 pKi = 6.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 218 1 2 3 0.9 C[C@@H]1CNC[C@H]2Cc3ccc(CO)cc3N12 10.1016/j.bmcl.2005.05.074
118729244 120660 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402662 120660 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547029 120660 0 None -1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
122188579 123158 0 None -1479 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
CHEMBL3612940 123158 0 None -1479 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
16062137 97684 0 None -125 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271419 97684 0 None -125 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
44298186 101684 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 458 4 1 5 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cc1C)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL299506 101684 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 458 4 1 5 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cc1C)CC2 10.1016/s0960-894x(00)00364-4
44298120 194977 0 None -158 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1ccc2c(c1Br)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
CHEMBL54775 194977 0 None -158 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1ccc2c(c1Br)CCN2C(=O)Nc1ccc(Oc2cccnc2C)nc1 10.1016/s0960-894x(00)00364-4
44323840 206549 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 9 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)=O)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL88809 206549 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 586 12 3 9 2.7 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C(C)=O)cc1 10.1016/S0960-894X(96)00503-3
155519891 170369 0 None 2 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 249 2 1 4 1.9 COc1cc(OC)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
CHEMBL4447975 170369 0 None 2 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 249 2 1 4 1.9 COc1cc(OC)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
155526977 171097 0 None 10 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 221 2 1 3 2.3 CC[C@H]1c2cc(OC)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4458099 171097 0 None 10 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 221 2 1 3 2.3 CC[C@H]1c2cc(OC)ccc2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
153287541 172171 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 279 1 0 2 3.9 CN1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4473697 172171 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 279 1 0 2 3.9 CN1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
153287539 176050 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3ccc(-c4ccccc4)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4591008 176050 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 265 1 1 2 3.6 C[C@@]12COc3ccc(-c4ccccc4)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
11465413 88014 0 None -125 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.7 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234494 88014 0 None -125 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.7 COc1ccc(N2Cc3cc(Cl)cc(Cl)c3C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.10.029
11305844 88147 0 None -630 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 466 6 0 4 5.1 COc1ccc(N2Cc3cc(F)cc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL234739 88147 0 None -630 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 466 6 0 4 5.1 COc1ccc(N2Cc3cc(F)cc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10368204 86735 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4ccc(F)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232047 86735 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4ccc(F)cc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
2337 3232 77 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
50 3232 77 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
5002 3232 77 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
CHEMBL716 3232 77 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
DB01224 3232 77 None -15 63 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
76325516 105704 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 280 4 1 3 3.7 O=c1cc(CCCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
CHEMBL3126299 105704 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranesDisplacement of [3H]LSD from human 5HT2B receptor expressed in stable HEK cells membranes
ChEMBL 280 4 1 3 3.7 O=c1cc(CCCc2ccccc2)oc2cccc(O)c12 10.1021/acs.jnatprod.5b00118
18357724 196574 0 None -31 3 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2ccc(C(F)(F)F)cc21 10.1016/s0960-894x(00)00365-6
CHEMBL56405 196574 0 None -31 3 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2ccc(C(F)(F)F)cc21 10.1016/s0960-894x(00)00365-6
162645563 179666 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2ccc(C(F)(F)F)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4743625 179666 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 348 4 1 3 4.7 O=c1cc(CCCc2ccc(C(F)(F)F)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
162648564 179897 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2ccc(Cl)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4746138 179897 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 314 4 1 3 4.3 O=c1cc(CCCc2ccc(Cl)cc2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
162666438 182246 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 298 4 1 3 3.8 O=c1cc(CCCc2cccc(F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
CHEMBL4783824 182246 0 None - 1 Human 5.6 pKi = 5.6 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 298 4 1 3 3.8 O=c1cc(CCCc2cccc(F)c2)oc2cccc(O)c12 10.1016/j.bmcl.2020.127511
44298126 101568 0 None -158 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c(Cl)cccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL298696 101568 0 None -158 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c(Cl)cccc32)cn1 10.1016/s0960-894x(00)00364-4
10085260 170603 0 None -66 5 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
CHEMBL445106 170603 0 None -66 5 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]- rauwolscine as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
71086303 160786 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4114493 160786 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
117209965 185223 1 None -10 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 185223 1 None -10 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
46914775 15398 0 None 3 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214959 15398 0 None 3 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
127035062 136426 0 None -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3735756 136426 0 None -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
127035062 136426 0 None -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 136426 0 None -4 19 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
15011385 161528 4 None -1 4 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 3 1 2 2.6 CN(C)CCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL412876 161528 4 None -1 4 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 244 3 1 2 2.6 CN(C)CCc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
45378936 199483 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591940 199483 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
70695555 77932 1 None -14 3 Human 5.6 pKi = 5.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@H]1CNC[C@@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL2096711 77932 1 None -14 3 Human 5.6 pKi = 5.6 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 188 0 1 2 1.4 C[C@H]1CNC[C@@H]2Cc3ccccc3N12 10.1016/j.bmcl.2005.05.074
168286277 191591 0 None -3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 468 3 2 3 6.5 Ic1ccc(Nc2nc3ccccc3c3[nH]c(C4CCCCC4)nc23)cc1 10.1021/acs.jmedchem.2c01170
CHEMBL5195535 191591 0 None -3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 468 3 2 3 6.5 Ic1ccc(Nc2nc3ccccc3c3[nH]c(C4CCCCC4)nc23)cc1 10.1021/acs.jmedchem.2c01170
1599 2326 50 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2326 50 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2326 50 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2326 50 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2326 50 None -144 16 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
46914771 15379 0 None 12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214831 15379 0 None 12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
165193 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3165 68 None -72 43 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4209 3141 75 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
4893 3141 75 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
503 3141 75 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
5385 3141 75 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
CHEMBL2 3141 75 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
DB00457 3141 75 None -758 34 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 nan
10085260 170603 0 None -66 5 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
CHEMBL445106 170603 0 None -66 5 Human 6.6 pKi = 6.6 Binding
Binding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligandBinding ability of compound at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT 2B as radioligand
ChEMBL 283 1 1 3 2.2 COc1cc(Br)c2c3c1C[C@H](N)C[C@@H]3CO2 10.1021/jm980076u
135433933 177014 1 None -2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL463249 177014 1 None -2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
136118728 93032 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442273 93032 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
90181059 160207 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL4109801 160207 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
10472143 119251 0 None -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 119251 0 None -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
59757153 106316 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1-c1ccccc1C2 10.1016/j.bmc.2013.10.010
CHEMBL3092762 106316 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1-c1ccccc1C2 10.1016/j.bmc.2013.10.010
CHEMBL3139190 106316 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 251 1 2 1 1.7 NC(N)=NC(=O)c1cccc2c1-c1ccccc1C2 10.1016/j.bmc.2013.10.010
118464427 138309 0 None 15 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 138309 0 None 15 7 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
118709750 113513 0 None -24 9 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
CHEMBL3321791 113513 0 None -24 9 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
44453652 155431 0 None 4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 1 1 3 2.8 Cc1nc2c(c(-c3ccc(Cl)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL403902 155431 0 None 4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 273 1 1 3 2.8 Cc1nc2c(c(-c3ccc(Cl)cc3)n1)CCNCC2 10.1016/j.bmcl.2008.01.090
73349361 92519 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432058 92519 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
136118636 76285 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058696 76285 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cc(Br)ccc12 10.1016/j.bmc.2013.09.011
43229249 140792 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
CHEMBL3818989 140792 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
25067564 201277 0 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 201277 0 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
56658157 65639 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 348 7 0 3 4.6 c1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834258 65639 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 348 7 0 3 4.6 c1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
43229249 140792 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
CHEMBL3818989 140792 1 None -70 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
44582706 186973 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 417 10 1 5 4.0 COc1ccc(CCN2CCC(C(O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
CHEMBL490633 186973 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 417 10 1 5 4.0 COc1ccc(CCN2CCC(C(O)c3cccc(OCCF)c3OC)CC2)cc1 10.1016/j.bmc.2009.03.021
3035850 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1039/D1MD00167A
457 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1039/D1MD00167A
CHEMBL431733 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1039/D1MD00167A
DB12885 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1039/D1MD00167A
3035850 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
457 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
CHEMBL431733 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
DB12885 948 73 None -15135 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.6b01183
145973771 164695 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 164695 0 None -3 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
21138 98423 39 None -6 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 98423 39 None -6 7 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
46914486 15388 0 None 13 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214894 15388 0 None 13 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
124087 1377 114 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1377 114 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1377 114 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1377 114 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1377 114 None -5 15 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
118055191 177291 0 None -31 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 280 0 1 2 2.7 CC1(C)CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4636977 177291 0 None -31 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 280 0 1 2 2.7 CC1(C)CN2CCNCc3ccc(Br)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL5074190 214291 0 None -112 9 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
11701315 199266 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590331 199266 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)N1CCNCC1NC2=O 10.1016/j.bmcl.2009.12.014
44554393 18515 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1275630 18515 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL4748908 214012 1 None -3 12 Human 6.6 pKi = 6.6 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
49783415 17646 0 None -3890 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17646 0 None -3890 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
136118647 76291 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.2 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058702 76291 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.2 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
1530 2169 50 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2169 50 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2169 50 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2169 50 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2169 50 None -19 21 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
122178707 121347 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OCC1CC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581252 121347 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OCC1CC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
11233293 84133 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 310 1 1 2 2.9 CC1(c2cc3c(c(C(F)(F)F)c2)C(=O)N2CCNC[C@@H]32)CC1 10.1021/jm0612968
CHEMBL220833 84133 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 310 1 1 2 2.9 CC1(c2cc3c(c(C(F)(F)F)c2)C(=O)N2CCNC[C@@H]32)CC1 10.1021/jm0612968
16115267 84764 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL223272 84764 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
71461049 82946 0 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181187 82946 0 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 364 6 0 4 4.9 CCCN1CCC(COc2nc3c(OC)cccc3c3ccccc23)CC1 10.1021/jm300943r
56665074 65634 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1cccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
CHEMBL1834253 65634 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1cccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
CHEMBL4748908 214012 1 None -3 12 Human 6.5 pKi = 6.5 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
155534799 176488 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysis
ChEMBL 416 7 1 6 2.7 O=c1c2cc(Cl)ccc2oc2ccc(CN3CCN(CCOCCO)CC3)cc12 10.1016/j.bmcl.2019.126679
CHEMBL4471059 176488 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysis
ChEMBL 416 7 1 6 2.7 O=c1c2cc(Cl)ccc2oc2ccc(CN3CCN(CCOCCO)CC3)cc12 10.1016/j.bmcl.2019.126679
CHEMBL4596904 176488 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysisDisplacement of [125I](+/-)DOI from recombinant human 5-HT2B receptor after 60 mins by radiometric scintillation analysis
ChEMBL 416 7 1 6 2.7 O=c1c2cc(Cl)ccc2oc2ccc(CN3CCN(CCOCCO)CC3)cc12 10.1016/j.bmcl.2019.126679
155535203 172017 0 None -7 6 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 403 5 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CCC3)C3CCC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
CHEMBL4471712 172017 0 None -7 6 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 403 5 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CCC3)C3CCC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
5353853 17954 47 None -23 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17954 47 None -23 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17954 47 None -23 15 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44409327 76603 0 None -128 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL206394 76603 0 None -128 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 261 3 1 4 1.9 CCO[C@@H](C)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
155531067 171595 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4465512 171595 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
71459604 83764 0 None -5 14 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83764 0 None -5 14 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
122187378 123000 0 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609143 123000 0 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
44455426 155125 0 None -4 12 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 155125 0 None -4 12 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
11288612 182587 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 267 2 1 3 3.0 c1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4788327 182587 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 267 2 1 3 3.0 c1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
145981805 166686 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 313 3 0 2 4.6 CN(C)CC/C=C1\c2ccc(Cl)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
CHEMBL4282729 166686 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 313 3 0 2 4.6 CN(C)CC/C=C1\c2ccc(Cl)cc2COc2ccccc21 10.1021/acsmedchemlett.8b00300
127048334 140575 1 None 13 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813796 140575 1 None 13 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccccc2Cl)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
135398737 955 93 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 955 93 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 955 93 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 955 93 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 955 93 None -2 92 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
29943048 67633 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL190699 67633 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
29943048 67633 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL190699 67633 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
1588 2311 27 None -6 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2311 27 None -6 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2311 27 None -6 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2311 27 None -6 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2311 27 None -6 44 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
11637931 120557 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343665 120557 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545814 120557 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 2 2 2.0 COC1(C)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
145993540 167310 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting method
ChEMBL 503 12 3 11 2.2 NCCCCNC(=O)COc1ccc(CCCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1 10.1039/C7MD00247E
CHEMBL4294350 167310 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEKT cells after 90 mins by scintillation counting method
ChEMBL 503 12 3 11 2.2 NCCCCNC(=O)COc1ccc(CCCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1 10.1039/C7MD00247E
127048335 140567 1 None 15 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813726 140567 1 None 15 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccccc2Br)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
11502243 189482 48 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmc.2019.02.044
CHEMBL513994 189482 48 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of 5-HT2B receptor (unknown origin)Inhibition of 5-HT2B receptor (unknown origin)
ChEMBL 401 4 1 6 4.4 N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F 10.1016/j.bmc.2019.02.044
146709966 175755 0 None 338 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4583909 175755 0 None 338 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 241 1 1 2 3.4 CC[C@H]1c2ccc3ccccc3c2OC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
72734865 106288 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Nc1ccccc1O2 10.1016/j.bmc.2013.10.010
CHEMBL3092756 106288 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Nc1ccccc1O2 10.1016/j.bmc.2013.10.010
CHEMBL3139103 106288 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 268 1 3 3 2.0 NC(N)=NC(=O)c1ccc2c(c1)Nc1ccccc1O2 10.1016/j.bmc.2013.10.010
135509961 136107 2 None -3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
CHEMBL373245 136107 2 None -3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 225 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(Cl)c21 10.1021/jm050663x
10623020 32370 0 None -12 2 Human 8.4 pKi = 8.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cnccc3C)c1)CC2 10.1021/jm990388c
CHEMBL14111 32370 0 None -12 2 Human 8.4 pKi = 8.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 441 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cnccc3C)c1)CC2 10.1021/jm990388c
18475630 101869 0 None 19 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 330 2 2 3 4.7 Cc1cc2cc(NC(=O)Nc3ccnc4ccccc34)ccc2n1C 10.1016/s0960-894x(01)00343-2
CHEMBL300835 101869 0 None 19 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 330 2 2 3 4.7 Cc1cc2cc(NC(=O)Nc3ccnc4ccccc34)ccc2n1C 10.1016/s0960-894x(01)00343-2
10690185 161730 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 365 3 1 3 4.5 CC(C)Oc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL41389 161730 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 365 3 1 3 4.5 CC(C)Oc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
1621 2413 17 None -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2413 17 None -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2413 17 None -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2413 17 None -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2413 17 None -19 45 Human 7.5 pKi = 7.5 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
2600 3750 74 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3750 74 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3750 74 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3750 74 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3750 74 None -1 13 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
118729264 120673 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402675 120673 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547136 120673 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
118729248 120677 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402664 120677 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547150 120677 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Br)cc2)C1 10.1016/j.bmc.2015.01.060
16062788 97445 0 None -50 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.6 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL270188 97445 0 None -50 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 333 3 1 3 3.6 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
16062781 155155 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 311 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL402357 155155 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 311 2 1 3 3.6 Fc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
127036932 137323 0 None 1 22 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 137323 0 None 1 22 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
44581973 175577 0 None -14 10 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458002 175577 0 None -14 10 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
73346042 91805 5 None -3019 17 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91805 5 None -3019 17 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
44451429 155743 3 None -21 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 226 1 1 3 1.9 O=[N+]([O-])c1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL405829 155743 3 None -21 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 226 1 1 3 1.9 O=[N+]([O-])c1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
89901929 120678 0 None -38 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402665 120678 0 None -38 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547151 120678 0 None -38 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
89901938 120687 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402684 120687 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547177 120687 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
145978113 163813 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 207 2 1 3 1.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4206418 163813 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 207 2 1 3 1.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
11312820 136309 1 None -8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL373402 136309 1 None -8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.2 C[C@H]1CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
46914621 15389 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
CHEMBL1214895 15389 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1cccc(CN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1021/jm100639f
122187375 122997 0 None 5 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 443 5 0 5 5.6 CCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609140 122997 0 None 5 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 443 5 0 5 5.6 CCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
4211 57792 83 None -2 4 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57792 83 None -2 4 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
11737032 84987 0 None -10 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223896 84987 0 None -10 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 222 0 1 2 1.4 O=C1c2c(Cl)cccc2C2CNCCN12 10.1021/jm0612968
44316017 205429 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80366 205429 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 228 2 1 2 2.2 C[C@H](N)CN1CCc2cc(F)c(Cl)cc21 10.1016/j.bmcl.2003.05.001
6761 67770 19 None -7 18 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67770 19 None -7 18 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
59752584 181471 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)c(Cl)c1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4764808 181471 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)c(Cl)c1)CCNCC2 10.1016/j.bmcl.2020.127669
118717213 120553 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 323 4 3 2 2.5 CCCCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343664 120553 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 323 4 3 2 2.5 CCCCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545802 120553 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 323 4 3 2 2.5 CCCCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
10244831 194864 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 309 3 2 3 4.6 CSc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
CHEMBL54062 194864 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 309 3 2 3 4.6 CSc1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
9888804 194968 4 None -63 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/j.bmcl.2005.08.004
CHEMBL54719 194968 4 None -63 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/j.bmcl.2005.08.004
10811153 169095 0 None -7 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 403 3 1 3 5.1 CSc1cc2c(cc1C(F)(F)C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
CHEMBL44015 169095 0 None -7 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
ChEMBL 403 3 1 3 5.1 CSc1cc2c(cc1C(F)(F)C(F)(F)F)N(C(=O)Nc1cccnc1)CC2 10.1021/jm970741j
44298173 195470 0 None -31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL55331 195470 0 None -31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 394 3 1 4 5.1 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cnccc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298236 195939 0 None -19 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 3 1 4 5.4 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(C)c1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL55964 195939 0 None -19 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 3 1 4 5.4 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)c(C)c1)CC2 10.1016/s0960-894x(00)00364-4
10435572 150076 0 None -12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cccc(F)c4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL395098 150076 0 None -12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cccc(F)c4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
50878551 90716 61 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90716 61 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
9888804 194968 4 None -63 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL54719 194968 4 None -63 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 428 4 1 4 5.0 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nc1)CC2 10.1016/s0960-894x(00)00365-6
11121216 30108 0 None -154 14 Human 6.5 pKi = 6.5 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 30108 0 None -154 14 Human 6.5 pKi = 6.5 Binding
Binding affinities towards 5-hydroxytryptamine 2B receptorBinding affinities towards 5-hydroxytryptamine 2B receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
3845148 65632 1 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 320 5 0 3 3.8 c1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834251 65632 1 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 320 5 0 3 3.8 c1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
16063181 155409 0 None -34 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL403764 155409 0 None -34 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 319 3 1 3 3.5 Fc1ccc(-c2nc(Cc3ccccc3)nc3c2CCNC3)cc1 10.1016/j.bmcl.2008.01.090
142601337 185946 0 None -97 5 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4869695 185946 0 None -97 5 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
145990659 166901 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 273 1 4 6 1.7 NC1=NC2(CCCCC2)NC(Nc2cccc(O)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4286819 166901 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 273 1 4 6 1.7 NC1=NC2(CCCCC2)NC(Nc2cccc(O)c2)=N1 10.1021/acsmedchemlett.8b00300
9906447 195554 2 None -4365 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5HT2B receptorBinding affinity to human recombinant 5HT2B receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031738 195554 2 None -4365 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5HT2B receptorBinding affinity to human recombinant 5HT2B receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 195554 2 None -4365 13 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5HT2B receptorBinding affinity to human recombinant 5HT2B receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
9909089 186944 0 None -2511 7 Human 6.5 pKi = 6.5 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL490417 186944 0 None -2511 7 Human 6.5 pKi = 6.5 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10217207 72083 0 None -398 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL197807 72083 0 None -398 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 463 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
10288601 72155 0 None -100 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 465 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198007 72155 0 None -100 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 465 7 0 5 4.2 COc1ccc(N2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
50898777 56410 0 None -2951 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632158 56410 0 None -2951 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
44414105 138160 0 None -79 2 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 488 7 0 4 5.9 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL376962 138160 0 None -79 2 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 488 7 0 4 5.9 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCC(C)(C)CC1 10.1016/j.bmcl.2006.05.034
19356259 102002 0 None -158 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL301784 102002 0 None -158 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Cl)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
44298192 168126 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 472 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(I)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL433060 168126 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 472 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(I)ccc32)cn1 10.1016/s0960-894x(00)00364-4
187 3363 18 None -288 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 10.1016/S0960-894X(96)00503-3
3693566 3363 18 None -288 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 10.1016/S0960-894X(96)00503-3
CHEMBL88402 3363 18 None -288 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 10.1016/S0960-894X(96)00503-3
11766873 206719 0 None -31 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 558 11 3 8 2.8 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL89967 206719 0 None -31 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 558 11 3 8 2.8 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C)cc1 10.1016/S0960-894X(96)00503-3
18931123 207206 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 601 12 4 9 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL92809 207206 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 601 12 4 9 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/S0960-894X(96)00503-3
153287567 172360 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 292 1 1 2 4.3 Cc1ccc(N2C[C@@]3(C)NCC[C@H]3c3cc(C)ccc32)cc1 10.1021/acsmedchemlett.9b00225
CHEMBL4476396 172360 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 292 1 1 2 4.3 Cc1ccc(N2C[C@@]3(C)NCC[C@H]3c3cc(C)ccc32)cc1 10.1021/acsmedchemlett.9b00225
153287557 176055 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 420 1 1 2 5.2 C[C@@]12CN(c3ccc(Br)cc3)c3ccc(Br)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4591108 176055 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 420 1 1 2 5.2 C[C@@]12CN(c3ccc(Br)cc3)c3ccc(Br)cc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
11463745 151764 0 None -79 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 400 6 0 4 4.4 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.029
CHEMBL396505 151764 0 None -79 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 400 6 0 4 4.4 COc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.10.029
11750162 151789 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 408 6 0 4 4.6 COc1ccc(N2Cc3cc(C)cc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL396527 151789 0 None -100 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 408 6 0 4 4.6 COc1ccc(N2Cc3cc(C)cc(C)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
179 399 115 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
2159 399 115 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
963 399 115 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
CHEMBL243712 399 115 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
DB06288 399 115 None -17 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1021/jm070516u
10440 2662 20 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2662 20 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2662 20 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
155531067 171595 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4465512 171595 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 369 7 3 6 3.3 Nc1nc(NCCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
155558626 174737 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
CHEMBL4561016 174737 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5HT2B stably expressed in HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting analysis
ChEMBL 355 6 3 6 2.9 Nc1nc(NCCc2ccccc2)nc(-c2cc(Cl)ccc2CO)n1 10.1021/acs.jmedchem.9b00869
44243470 89069 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334981 89069 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365395 89069 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
18931217 206767 0 None -39 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 623 12 4 10 1.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(S(N)(=O)=O)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90267 206767 0 None -39 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 623 12 4 10 1.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(S(N)(=O)=O)cc1 10.1016/S0960-894X(96)00503-3
44439167 90528 0 None -316 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238732 90528 0 None -316 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
71062790 160029 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4108274 160029 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
44420683 84104 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 0 1 2 2.6 CC1(C)CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
CHEMBL220789 84104 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 284 0 1 2 2.6 CC1(C)CN2C(=O)c3c(cccc3C(F)(F)F)[C@@H]2CN1 10.1021/jm0612968
1355 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
142 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
CHEMBL478 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
DB12110 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
11151653 91072 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397896 91072 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 Cc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
1355 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
142 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
CHEMBL478 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
DB12110 1998 88 None -1 16 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2005.10.029
CHEMBL5084249 214882 0 None -38 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
1704 3496 85 None -10 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
4331799 3496 85 None -10 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
CHEMBL1334465 3496 85 None -10 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
118055337 177347 0 None -28 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 220 0 1 2 2.0 CC1(C)CN2CCNCc3ccc(F)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4637882 177347 0 None -28 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 220 0 1 2 2.0 CC1(C)CN2CCNCc3ccc(F)c1c32 10.1016/j.bmcl.2019.126929
44582675 189677 0 None -5 15 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189677 0 None -5 15 Human 6.5 pKi = 6.5 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
3336 94972 30 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1021/jm100600y
CHEMBL1405922 94972 30 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1021/jm100600y
CHEMBL254832 94972 30 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1021/jm100600y
16573 177595 34 None -16 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 177595 34 None -16 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
168273532 190161 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 450 3 2 3 7.8 Clc1ccc(Nc2nc3ccccc3c3[nH]c([C@@H]4C[C@@H]5CCC[C@@H](C5)C4)nc23)cc1Cl 10.1021/acs.jmedchem.2c01170
CHEMBL5174205 190161 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assayDisplacement of [3H]-LSD from human 5HT2B expressed in human HEK293 cell membrane incubated for 90 mins by radioligand binding assay
ChEMBL 450 3 2 3 7.8 Clc1ccc(Nc2nc3ccccc3c3[nH]c([C@@H]4C[C@@H]5CCC[C@@H](C5)C4)nc23)cc1Cl 10.1021/acs.jmedchem.2c01170
23290944 81797 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 81797 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
6075 150084 42 None -8 16 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150084 42 None -8 16 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
44247568 82145 55 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
CHEMBL2170062 82145 55 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 337 5 0 5 3.0 Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1 10.1021/jm3007323
16118923 60116 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642866 60116 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739656 60116 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
11695000 89042 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 89042 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 89042 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
122178706 121346 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581251 121346 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
3038495 705 37 None -22 19 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm100600y
7625 705 37 None -22 19 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm100600y
CHEMBL25236 705 37 None -22 19 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm100600y
11948707 166143 0 None -83 13 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 166143 0 None -83 13 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
5624 32663 14 None 5 10 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32663 14 None 5 10 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32663 14 None 5 10 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
56675413 65640 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccccc1CCCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
CHEMBL1834259 65640 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccccc1CCCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
134143302 145291 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 503 9 5 9 0.6 CC(=O)NCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3913293 145291 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 503 9 5 9 0.6 CC(=O)NCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
90181065 160788 0 None 5 2 Mouse 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@@H](COc2cccc(Cl)c2)C1 nan
CHEMBL4114519 160788 0 None 5 2 Mouse 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@@H](COc2cccc(Cl)c2)C1 nan
155566272 175764 0 None 4 5 Human 6.5 pKi = 6.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 543 8 3 8 5.1 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CSc2ccccc2F)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4584140 175764 0 None 4 5 Human 6.5 pKi = 6.5 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 543 8 3 8 5.1 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CSc2ccccc2F)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL5089613 215193 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL None None None C=C[C@H]1CN2CCc3c([nH]c4cccc(O)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
16115654 136949 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374562 136949 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 270 0 1 2 2.1 Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
44451373 96306 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2ccc3c(c2o1)CCNCC3 10.1016/j.bmc.2007.12.009
CHEMBL261490 96306 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2ccc3c(c2o1)CCNCC3 10.1016/j.bmc.2007.12.009
50878551 90716 61 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90716 61 None -1 18 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
118706296 120499 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 308 2 3 2 1.3 CC(=O)NC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310119 120499 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 308 2 3 2 1.3 CC(=O)NC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545441 120499 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 308 2 3 2 1.3 CC(=O)NC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
134143536 145492 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3914843 145492 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
71459269 82931 0 None -1479 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
CHEMBL2181166 82931 0 None -1479 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
58911532 91075 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397899 91075 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 2 1 2 1.6 CCCc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
11176570 91091 1 None -8 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397915 91091 1 None -8 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
56661666 65641 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1cccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
CHEMBL1834260 65641 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1cccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)c1 10.1016/j.bmcl.2011.08.029
11150514 84848 0 None -3 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@H]2CNCCN12 10.1021/jm0612968
CHEMBL223584 84848 0 None -3 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@H]2CNCCN12 10.1021/jm0612968
16071847 60115 0 None -229 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642865 60115 0 None -229 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739655 60115 0 None -229 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
11195293 91059 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397883 91059 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@]12CNCCN1C(=O)c1ccccc1C2 10.1016/j.bmcl.2013.04.061
90181070 160513 0 None 1 3 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ccnc(OC[C@H]2CN(CC(=O)N3c4ccccc4CC3C)CCO2)c1 nan
CHEMBL4112412 160513 0 None 1 3 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ccnc(OC[C@H]2CN(CC(=O)N3c4ccccc4CC3C)CCO2)c1 nan
136118621 76224 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2058420 76224 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
4943 193393 105 None 1 2 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
CHEMBL526 193393 105 None 1 2 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O nan
135399666 168739 7 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL437314 168739 7 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
46884034 7897 0 None -870 2 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 347 3 2 2 3.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1F)N1CCNCC1 10.1016/j.bmcl.2010.01.107
CHEMBL1090397 7897 0 None -870 2 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 347 3 2 2 3.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1F)N1CCNCC1 10.1016/j.bmcl.2010.01.107
118055294 177450 0 None -24 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 204 1 1 3 1.2 COc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4639115 177450 0 None -24 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 204 1 1 3 1.2 COc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
56682068 65642 0 None 16 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834261 65642 0 None 16 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 378 8 0 4 4.6 COc1ccc(CCCCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
4189 206899 96 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206899 96 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206899 96 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
136118651 76295 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058706 76295 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
127052458 140715 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140715 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
9881119 205450 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
CHEMBL80482 205450 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 232 2 1 3 1.7 C[C@H](N)CN1CCc2ccc3c(c21)CCCO3 10.1016/j.bmcl.2003.05.001
117209864 186010 1 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4870675 186010 1 None -1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
127052458 140715 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140715 0 None -35 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
168284710 191569 0 None -17 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5195241 191569 0 None -17 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccc(Br)cc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
135398745 2893 112 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2893 112 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2893 112 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2893 112 None -5 66 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
127035066 136396 0 None 7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735434 136396 0 None 7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 507 14 0 7 5.2 COc1ccc(OC)c(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
156021327 178109 0 None -33 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 224 0 1 3 1.6 Clc1ccc2c3c1OCCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4648457 178109 0 None -33 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 224 0 1 3 1.6 Clc1ccc2c3c1OCCN3CCNC2 10.1016/j.bmcl.2019.126929
132075278 162620 0 None -6 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4169752 162620 0 None -6 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
2683 102861 25 None -501 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102861 25 None -501 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102861 25 None -501 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
3598 187797 76 None -2 7 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
CHEMBL496 187797 76 None -2 7 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl nan
136118635 76283 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
CHEMBL2058694 76283 0 None 5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 321 1 3 2 2.3 O=C1NC(=S)N/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
16115148 84810 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 206 0 1 2 0.9 O=C1c2c(F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL223469 84810 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 206 0 1 2 0.9 O=C1c2c(F)cccc2C2CNCCN12 10.1021/jm0612968
156014235 177154 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 240 0 1 3 2.4 Clc1ccc2c3c1SCCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4634836 177154 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 240 0 1 3 2.4 Clc1ccc2c3c1SCCN3CCNC2 10.1016/j.bmcl.2019.126929
53324045 57041 0 None -9 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 57041 0 None -9 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
11253485 141953 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 204 0 2 3 0.5 O=C1c2c(O)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL387344 141953 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 204 0 2 3 0.5 O=C1c2c(O)cccc2C2CNCCN12 10.1021/jm0612968
44409101 141225 0 None -23 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 2 1 4 1.0 COCc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL383051 141225 0 None -23 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 2 1 4 1.0 COCc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
18735305 204910 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76301 204910 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 320 2 1 2 2.1 C[C@H](N)CN1CCc2cc(F)c(I)cc21 10.1016/j.bmcl.2003.05.001
44404883 72033 32 None -2 4 Human 7.4 pKi = 7.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197664 72033 32 None -2 4 Human 7.4 pKi = 7.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
44364215 39598 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1ccc2[nH]cc(C3CC3N)c2c1 10.1021/jm980318q
CHEMBL147434 39598 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1ccc2[nH]cc(C3CC3N)c2c1 10.1021/jm980318q
118464425 138284 0 None 3 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 138284 0 None 3 9 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
145976085 163641 0 None 2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204576 163641 0 None 2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
44407453 74374 0 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
CHEMBL202538 74374 0 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 349 5 1 3 5.0 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1Cl 10.1016/j.bmcl.2005.10.029
11163458 136543 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 2 1 2 2.8 CCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL373905 136543 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 2 1 2 2.8 CCCc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
49865831 16129 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 2 1 3 3.0 CCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224033 16129 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 2 1 3 3.0 CCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
132060720 162465 0 None 2 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 162465 0 None 2 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
11206703 91063 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
CHEMBL2397887 91063 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@@H]1CNC[C@H]2Cc3ccccc3C(=O)N12 10.1016/j.bmcl.2013.04.061
10528314 171857 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 469 3 1 3 6.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C(C)(C)C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL446942 171857 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 469 3 1 3 6.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C(C)(C)C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
240 941 43 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
2769 941 43 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
44279790 941 43 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
660 941 43 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL1729 941 43 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
CHEMBL560739 941 43 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
DB00604 941 43 None -6 25 Human 7.4 pKi = 7.4 Binding
Binding affinity to human serotonin 5-HT2B receptorBinding affinity to human serotonin 5-HT2B receptor
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1016/j.bmcl.2013.05.018
18005120 194945 0 None -100 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 460 4 1 5 5.9 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL54560 194945 0 None -100 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 460 4 1 5 5.9 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298086 195196 0 None -39 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(Cl)c(C)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55079 195196 0 None -39 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 428 3 1 4 5.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(Cl)c(C)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
44298234 196712 0 None -25 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 462 3 1 4 6.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL56508 196712 0 None -25 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 462 3 1 4 6.2 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)c(Cl)c1)CC2 10.1016/s0960-894x(00)00364-4
10255548 86734 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4cc(Cl)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232046 86734 0 None -12 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 467 6 0 5 5.1 COc1ccc(N2Cc3c(c4cc(Cl)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
2726 916 68 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 916 68 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 916 68 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 916 68 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 916 68 None -19 73 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]DOI from 5HT2B receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
25235287 177692 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 302 0 1 2 4.5 Cc1nccc2c1C(C)(C)Nc1cc(Br)ccc1-2 10.1021/acs.jnatprod.9b01107
CHEMBL4642292 177692 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 302 0 1 2 4.5 Cc1nccc2c1C(C)(C)Nc1cc(Br)ccc1-2 10.1021/acs.jnatprod.9b01107
136188797 57292 1 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
CHEMBL1651094 57292 1 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
136030744 57291 1 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
CHEMBL1651093 57291 1 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
11288140 84740 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 213 0 1 3 0.7 N#Cc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL223090 84740 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 213 0 1 3 0.7 N#Cc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
46830177 8029 30 None -4365 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1091105 8029 30 None -4365 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
118055319 177502 0 None -20 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 1 1 2 2.6 FC(F)(F)CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
CHEMBL4639970 177502 0 None -20 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 1 1 2 2.6 FC(F)(F)CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
10050022 166332 0 None -39 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(C2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL427398 166332 0 None -39 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 462 7 0 4 5.4 COc1ccc(C2CCN(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
49850870 56359 0 None -3162 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631535 56359 0 None -3162 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
49850570 56442 0 None -2511 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 417 6 2 4 4.0 CCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632220 56442 0 None -2511 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 417 6 2 4 4.0 CCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
44298140 100531 0 None -79 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL291510 100531 0 None -79 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(C(F)(F)F)cc32)cn1 10.1016/s0960-894x(00)00364-4
18931172 106147 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1Cl 10.1016/S0960-894X(96)00503-3
CHEMBL313745 106147 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1Cl 10.1016/S0960-894X(96)00503-3
18931163 206752 0 None -50 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 569 11 3 9 2.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C#N)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90175 206752 0 None -50 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 569 11 3 9 2.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(C#N)cc1 10.1016/S0960-894X(96)00503-3
18931420 206823 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 628 12 3 9 3.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL90565 206823 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 628 12 3 9 3.4 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/S0960-894X(96)00503-3
127052465 140706 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
CHEMBL3817911 140706 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
10835585 101834 0 None -63 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(C(F)(F)F)ccc21 10.1016/s0960-894x(00)00365-6
CHEMBL300618 101834 0 None -63 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 414 4 1 4 4.7 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(C(F)(F)F)ccc21 10.1016/s0960-894x(00)00365-6
1836 2574 59 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2574 59 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2574 59 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2574 59 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2574 59 None -69 15 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
10597140 63015 0 None -251 6 Human 5.4 pKi = 5.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 400 5 0 3 4.5 CC1CCN(CC[C@H]2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL1788231 63015 0 None -251 6 Human 5.4 pKi = 5.4 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligandBinding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand
ChEMBL 400 5 0 3 4.5 CC1CCN(CC[C@H]2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
1703 3493 97 None -158 6 Human 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 319 2 2 5 3.7 O=C(Nc1ccnc2c1nccc2)Nc1ccc2c(c1)oc(n2)C 10.1016/s0960-894x(01)00343-2
6604926 3493 97 None -158 6 Human 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 319 2 2 5 3.7 O=C(Nc1ccnc2c1nccc2)Nc1ccc2c(c1)oc(n2)C 10.1016/s0960-894x(01)00343-2
CHEMBL291536 3493 97 None -158 6 Human 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 319 2 2 5 3.7 O=C(Nc1ccnc2c1nccc2)Nc1ccc2c(c1)oc(n2)C 10.1016/s0960-894x(01)00343-2
44343212 9806 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.
ChEMBL 400 5 0 3 4.5 CC1CCN(CCC2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL114012 9806 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.Binding affinity towards 5-hydroxytryptamine 2B receptor (human cloned receptor) in HEK 293 cells using [3H]5-HT as radioligand.
ChEMBL 400 5 0 3 4.5 CC1CCN(CCC2CCCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
49865890 16150 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 1 1 3 3.5 Cc1ccccc1NC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224106 16150 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 1 1 3 3.5 Cc1ccccc1NC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
57799324 89063 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337501 89063 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365359 89063 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
11312173 182087 0 None -3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 2 1 3 3.1 Fc1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
CHEMBL4782005 182087 0 None -3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 285 2 1 3 3.1 Fc1ccc(-c2c3c(nn2C2CCC2)CCNCC3)cc1 10.1016/j.bmcl.2020.127669
127034715 136369 0 None 35 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735261 136369 0 None 35 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 537 15 0 8 5.2 COc1ccc(CCN(CCCc2cc(OC)c(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
107715 200922 22 None -14 20 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 200922 22 None -14 20 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 200922 22 None -14 20 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
189 3466 39 None -5 17 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm100600y
5163 3466 39 None -5 17 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm100600y
CHEMBL297784 3466 39 None -5 17 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 10.1021/jm100600y
11694810 120513 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310123 120513 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545474 120513 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
11694810 120513 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3310123 120513 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545474 120513 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 281 1 3 2 1.3 CC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
10531 1408 21 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1408 21 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1408 21 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1408 21 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1408 21 None -15 24 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
118706301 120512 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 265 1 2 1 2.2 CC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3310122 120512 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 265 1 2 1 2.2 CC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
CHEMBL3545473 120512 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 265 1 2 1 2.2 CC1c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.05.027
168293874 192155 0 None 5 11 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192155 0 None 5 11 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
145988313 167211 0 None 104 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 167211 0 None 104 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
168268877 189946 0 None 1 12 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189946 0 None 1 12 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
127035064 136446 0 None 23 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3735911 136446 0 None 23 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
135 2515 43 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2515 43 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2515 43 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2515 43 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2515 43 None -3 58 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
11681111 120558 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343666 120558 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545815 120558 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 309 3 2 2 2.4 CCC1(OC)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
16062783 154998 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 323 3 1 4 3.5 COc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL401509 154998 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 323 3 1 4 3.5 COc1ccc(-c2nc(C3CCCC3)nc3c2CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
14049689 198420 11 None 20 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
CHEMBL577294 198420 11 None 20 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 1541 28 21 42 -12.4 CC(O)COC[C@H]1O[C@@H]2O[C@@H]3[C@@H](COCC(C)O)O[C@H](O[C@@H]4[C@@H](COCC(C)O)O[C@H](O[C@@H]5[C@@H](COCC(C)O)O[C@H](O[C@@H]6[C@@H](COCC(C)O)O[C@H](O[C@@H]7[C@@H](COCC(C)O)O[C@H](O[C@@H]8[C@@H](COCC(C)O)O[C@H](O[C@H]1[C@H](O)[C@H]2O)[C@H](O)[C@H]8O)[C@H](O)[C@H]7O)[C@H](O)[C@H]6O)[C@H](O)[C@H]5O)[C@H](O)[C@H]4O)[C@H](O)[C@H]3O nan
58911653 91087 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397911 91087 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 244 1 1 2 1.5 CCc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
57799306 89080 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337493 89080 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365469 89080 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 222 0 2 2 1.1 O=C1N[C@H]2CNC[C@@H]2c2cccc(Cl)c21 10.1016/j.bmcl.2012.10.091
9899500 67860 0 None -14 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.11.083
CHEMBL191054 67860 0 None -14 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 236 0 1 2 2.4 Cc1c(Cl)ccc2c1N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.11.083
168281367 190877 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OCC3CC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5185086 190877 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 395 6 0 5 4.3 COc1cc2c(cc1OC)-c1c(OC)c(OCC3CC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
118729232 120649 0 None 9 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402655 120649 0 None 9 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547008 120649 0 None 9 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 5.0 CN(C)[C@H]1Cc2ccccc2[C@H](C2CCCCCCC2)C1 10.1016/j.bmc.2015.01.060
90188146 120672 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402674 120672 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547135 120672 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
16062912 155128 0 None -56 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 351 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL402164 155128 0 None -56 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 351 3 1 3 3.7 Fc1ccc(Cc2nc3c(c(-c4ccc(F)cc4)n2)CCNCC3)cc1 10.1016/j.bmcl.2008.01.090
71461050 82948 0 None -13 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181189 82948 0 None -13 5 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 352 5 0 3 5.0 CCCN1CCC(COc2nc3c(F)cccc3c3ccccc23)CC1 10.1021/jm300943r
45486891 196917 0 None -83 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL566379 196917 0 None -83 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
145974750 164731 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4217810 164731 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
127052465 140706 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
CHEMBL3817911 140706 0 None -10 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
89901924 120680 0 None -100 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402667 120680 0 None -100 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547153 120680 0 None -100 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
16062651 95616 0 None -13 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.1 CC(C)Cc1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL257944 95616 0 None -13 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 3 1 3 3.1 CC(C)Cc1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
132007291 148921 0 None -33 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 395 3 2 4 4.3 Fc1ccc(C#Cc2nc(NCc3cccc(Cl)c3)c3nc[nH]c3n2)cc1F 10.1021/acs.jmedchem.6b01183
CHEMBL3941980 148921 0 None -33 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 395 3 2 4 4.3 Fc1ccc(C#Cc2nc(NCc3cccc(Cl)c3)c3nc[nH]c3n2)cc1F 10.1021/acs.jmedchem.6b01183
1782 2501 84 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
241 2501 84 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
4168 2501 84 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
CHEMBL86 2501 84 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
DB01233 2501 84 None -3 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC nan
11171955 91064 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
CHEMBL2397888 91064 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.2 C[C@@H]1c2ccccc2C(=O)N2CCNC[C@@H]12 10.1016/j.bmcl.2013.04.061
16115515 137571 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 290 0 1 2 2.5 O=C1c2c(C(F)(F)F)ccc(Cl)c2[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL375575 137571 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 290 0 1 2 2.5 O=C1c2c(C(F)(F)F)ccc(Cl)c2[C@@H]2CNCCN12 10.1021/jm0612968
2775690 92982 53 None -15 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 92982 53 None -15 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT2B receptor (unknown origin)Binding affinity to 5-HT2B receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
11848624 89117 0 None 2 6 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL236587 89117 0 None 2 6 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
46230100 199296 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590531 199296 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
118717211 120552 0 None -33 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3343663 120552 0 None -33 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
CHEMBL3545801 120552 0 None -33 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 295 2 3 2 1.7 CCC1(O)c2ccccc2-c2ccc(C(=O)N=C(N)N)cc21 10.1016/j.bmc.2014.09.005
44451422 167401 2 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 199 0 1 1 2.2 Fc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL429689 167401 2 None -9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 199 0 1 1 2.2 Fc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
75201901 166401 19 None -301 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 166401 19 None -301 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
118729238 120653 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402659 120653 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547012 120653 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
118729240 120654 0 None -6 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402660 120654 0 None -6 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547013 120654 0 None -6 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmc.2015.01.060
46884098 8155 0 None -954 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 286 4 2 2 3.1 O=C(NCc1ccc(C2CCCCC2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1092029 8155 0 None -954 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT2B receptorBinding affinity to 5HT2B receptor
ChEMBL 286 4 2 2 3.1 O=C(NCc1ccc(C2CCCCC2)cc1)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
142601329 186493 5 None -63 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 186493 5 None -63 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
122187379 123001 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 441 5 0 5 5.3 C=CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609144 123001 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 441 5 0 5 5.3 C=CCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
122483223 138084 0 None -5 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3764650 138084 0 None -5 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765874 138084 0 None -5 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
122187382 123003 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCN1CC(c2ccccc2)c2cc(OC)c(OC)c3c2C1Cc1cc2c(cc1-3)OCO2 10.1016/j.bmcl.2015.07.012
CHEMBL3609147 123003 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 429 4 0 5 5.2 CCN1CC(c2ccccc2)c2cc(OC)c(OC)c3c2C1Cc1cc2c(cc1-3)OCO2 10.1016/j.bmcl.2015.07.012
137646281 157782 0 None -95 17 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157782 0 None -95 17 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
122178711 121351 0 None 1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OCc1ccc(Br)cc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581256 121351 0 None 1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 509 6 0 5 5.8 COc1cc2c(cc1OCc1ccc(Br)cc1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
46933845 16130 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224034 16130 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 336 1 1 3 3.9 O=C(NC1CCCCC1)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
11957541 1446 40 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
1229 1446 40 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
147 1446 40 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
170617 1446 40 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
CHEMBL6616 1446 40 None -2 16 Human 7.4 pKi = 7.4 Binding
Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.
ChEMBL 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 10.1021/jm9803525
25117676 200436 0 None -831 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598444 200436 0 None -831 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
53325242 57040 0 None -2 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 57040 0 None -2 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
21854226 124578 5 None -1 3 Human 6.4 pKi = 6.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 230 3 2 2 2.5 Oc1cccc2[nH]cc(CCN3CCCC3)c12 10.1016/j.bmcl.2005.06.104
CHEMBL364061 124578 5 None -1 3 Human 6.4 pKi = 6.4 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 230 3 2 2 2.5 Oc1cccc2[nH]cc(CCN3CCCC3)c12 10.1016/j.bmcl.2005.06.104
2286 3161 51 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3161 51 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3161 51 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3161 51 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3161 51 None -5 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
59752589 179802 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)cc1Cl)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4745055 179802 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 4.1 CC(C)n1nc2c(c1-c1ccc(Cl)cc1Cl)CCNCC2 10.1016/j.bmcl.2020.127669
11425677 182311 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 1 1 3 3.0 CC(C)(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4784424 182311 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 269 1 1 3 3.0 CC(C)(C)n1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
145975946 163896 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4207355 163896 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
2406 100376 89 None -27 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
CHEMBL290106 100376 89 None -27 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O nan
3198 205490 76 None -30 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205490 76 None -30 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205490 76 None -30 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
118055192 177009 0 None -46 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 188 0 1 2 1.7 CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
CHEMBL4632419 177009 0 None -46 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 188 0 1 2 1.7 CC1CN2CCNCc3cccc1c32 10.1016/j.bmcl.2019.126929
10947658 28671 0 None -39 16 Human 7.4 pKi = 7.4 Binding
Binding affinities against 5-hydroxytryptamine 2B receptorBinding affinities against 5-hydroxytryptamine 2B receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28671 0 None -39 16 Human 7.4 pKi = 7.4 Binding
Binding affinities against 5-hydroxytryptamine 2B receptorBinding affinities against 5-hydroxytryptamine 2B receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
44409095 76001 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 1 4 0.8 COc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL205671 76001 0 None -4 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 219 1 1 4 0.8 COc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
71618702 143357 0 None 1 4 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
CHEMBL3897835 143357 0 None 1 4 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
156014421 177181 0 None -12 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 3 1.4 [O-][S+]1CCN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4635293 177181 0 None -12 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 256 0 1 3 1.4 [O-][S+]1CCN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
25122654 200505 0 None -54 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
CHEMBL598851 200505 0 None -54 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
135476741 155501 11 None -7 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL404232 155501 11 None -7 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
117209962 184845 1 None -16 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184845 1 None -16 7 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
136118716 93030 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442271 93030 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
180 400 56 None -35 40 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 400 56 None -35 40 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 400 56 None -35 40 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 400 56 None -35 40 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 400 56 None -35 40 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
122178703 121343 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC(C)C)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581248 121343 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 383 5 0 5 4.3 COc1cc2c(cc1OC(C)C)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
127049980 140609 1 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccc(Br)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814485 140609 1 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 525 12 0 5 5.9 COc1ccc(CCN(CCCc2ccc(Br)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
134144970 150749 0 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 461 8 3 9 2.3 CCCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3956531 150749 0 None 4 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 461 8 3 9 2.3 CCCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
12901777 137973 32 None -7 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 188 0 1 2 0.8 O=C1c2ccccc2C2CNCCN12 10.1021/jm0612968
CHEMBL376455 137973 32 None -7 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 188 0 1 2 0.8 O=C1c2ccccc2C2CNCCN12 10.1021/jm0612968
44407337 74175 0 None -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202324 74175 0 None -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 265 5 1 3 3.4 C=CCN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
45378934 201623 0 None -8 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL605971 201623 0 None -8 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
135449090 189290 4 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL512332 189290 4 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
4595 176691 106 None 2 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL46 176691 106 None 2 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O nan
136118729 93033 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442274 93033 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
10150497 4043 47 None -223 4 Human 6.3 pKi = 6.3 Binding
Inhibition of human 5HT2B receptor expressed in CHO cellsInhibition of human 5HT2B receptor expressed in CHO cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
3240 4043 47 None -223 4 Human 6.3 pKi = 6.3 Binding
Inhibition of human 5HT2B receptor expressed in CHO cellsInhibition of human 5HT2B receptor expressed in CHO cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
CHEMBL392760 4043 47 None -223 4 Human 6.3 pKi = 6.3 Binding
Inhibition of human 5HT2B receptor expressed in CHO cellsInhibition of human 5HT2B receptor expressed in CHO cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
168 3951 15 None -3 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
6604042 3951 15 None -3 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
CHEMBL309760 3951 15 None -3 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 10.1016/j.bmcl.2003.05.001
10430183 205605 0 None -457 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL81728 205605 0 None -457 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human 5-HT2B receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
118055338 177161 0 None -57 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.4 CC1CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
CHEMBL4634942 177161 0 None -57 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 222 0 1 2 2.4 CC1CN2CCNCc3ccc(Cl)c1c32 10.1016/j.bmcl.2019.126929
56852956 112016 1 None -12 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112016 1 None -12 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
71618636 148861 0 None -7 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
CHEMBL3941579 148861 0 None -7 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
56665075 65635 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
CHEMBL1834254 65635 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 350 6 0 4 3.8 COc1ccc(CCN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmcl.2011.08.029
1547484 937 74 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 937 74 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 937 74 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 937 74 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 937 74 None -8 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44582678 181550 0 None -3 10 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 181550 0 None -3 10 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
136188797 57292 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
CHEMBL1651094 57292 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@H]1SC[C@](C)(C(=O)O)N1C 10.1021/np100588c
102 4096 48 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4096 48 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4096 48 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4096 48 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4096 48 None -93 50 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
24826787 91068 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397892 91068 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
24826869 91073 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397897 91073 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1ccc2c(c1)C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
145964159 164305 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4212435 164305 0 None 3 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
168281307 190782 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5183799 190782 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
56852956 112016 1 None -12 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112016 1 None -12 9 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by PDSP assayDisplacement of [3H]LSD from human 5-HT2B receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
11347858 137012 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 2 3 1.3 O=C1c2c(cc(CO)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL374659 137012 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 286 1 2 3 1.3 O=C1c2c(cc(CO)cc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
136030744 57291 1 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
CHEMBL1651093 57291 1 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 352 3 2 6 2.5 C[C@@H]1SC(c2ccccc2O)=N[C@H]1[C@@H]1SC[C@](C)(C(=O)O)N1C 10.1021/acs.jnatprod.7b00317
134149008 148437 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 353 3 3 8 -0.1 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)O)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL3938006 148437 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 353 3 3 8 -0.1 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)O)C[C@H]12 10.1021/acs.jmedchem.6b01183
16115521 84636 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc2c(cc1Cl)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL222466 84636 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc2c(cc1Cl)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
155566338 175887 0 None -446 6 Human 6.3 pKi = 6.3 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 405 4 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4587144 175887 0 None -446 6 Human 6.3 pKi = 6.3 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 405 4 4 8 1.4 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
134134668 144228 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 6 4 8 1.4 CCC(CC)Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL3904817 144228 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 6 4 8 1.4 CCC(CC)Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
2477 742 59 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
36 742 59 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
437 742 59 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
CHEMBL49 742 59 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
DB00490 742 59 None -13 29 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 nan
11666237 89083 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337496 89083 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365472 89083 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 236 0 2 2 1.4 Cc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
11609026 89098 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337500 89098 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365705 89098 0 None -3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.8 O=C1N[C@H]2CNC[C@@H]2c2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2012.10.091
44409031 74927 0 None -30 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@H]2Cc3ccc(Cl)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203230 74927 0 None -30 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 223 0 1 3 1.5 C[C@@H]1CNC[C@H]2Cc3ccc(Cl)nc3N12 10.1016/j.bmcl.2005.11.083
122178702 121342 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OCCF)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581247 121342 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OCCF)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
168295984 192196 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5204813 192196 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 431 6 0 5 5.0 COc1cc2c(cc1OC)-c1c(OC)c(OCc3ccccc3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
134155462 151085 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 339 3 3 8 -0.2 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL3959210 151085 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 339 3 3 8 -0.2 CN(C)c1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
10058473 20623 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2sccc12 10.1021/jm980692q
CHEMBL13086 20623 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptorCompound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor
ChEMBL 194 3 1 2 2.3 CN(C)CCc1c[nH]c2sccc12 10.1021/jm980692q
71681898 91060 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 0 2 1.0 CN1CCN2C(=O)c3ccccc3C[C@@H]2C1 10.1016/j.bmcl.2013.04.061
CHEMBL2397884 91060 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 0 2 1.0 CN1CCN2C(=O)c3ccccc3C[C@@H]2C1 10.1016/j.bmcl.2013.04.061
49865832 16131 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 3 1 3 3.3 CCCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224035 16131 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 310 3 1 3 3.3 CCCCNC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
136118618 76221 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058417 76221 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
56707820 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL4507323
9155 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL4507323
CHEMBL4548689 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL4507323
CHEMBL5306285 194560 0 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 486 7 2 9 3.2 C[C@H](NC(=O)c1cn(C2(C#N)CC2)cn1)C(=O)Nc1nc(-c2cccc(-c3ccn(C)n3)c2)cs1 10.6019/CHEMBL5303766
9859257 205100 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
CHEMBL77880 205100 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 218 2 1 3 1.3 C[C@H](N)CN1CCc2ccc3c(c21)CCO3 10.1016/j.bmcl.2003.05.001
2105 3032 37 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3032 37 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3032 37 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3032 37 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3032 37 None -28 33 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
71028 84332 25 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 216 1 2 2 2.4 COc1ccc2[nH]c3c(c2c1)CCNC3C 10.1021/jm100600y
CHEMBL221811 84332 25 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 216 1 2 2 2.4 COc1ccc2[nH]c3c(c2c1)CCNC3C 10.1021/jm100600y
25122652 200639 0 None -134 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
CHEMBL599663 200639 0 None -134 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
11653679 181167 1 None -75 11 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5HT2B receptorBinding affinity to human cloned 5HT2B receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 181167 1 None -75 11 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5HT2B receptorBinding affinity to human cloned 5HT2B receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
56707820 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL4507323
9155 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL4507323
CHEMBL4548689 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL4507323
56707820 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL5212743
9155 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL5212743
CHEMBL4548689 2890 39 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000354a HTR2B
ChEMBL 307 5 3 6 2.2 OCc1ccccc1c1nc(NCc2ccccc2)nc(n1)N 10.6019/CHEMBL5212743
5009938 15377 1 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 306 4 0 3 3.8 c1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214829 15377 1 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 306 4 0 3 3.8 c1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
11393128 182837 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 3.8 CC(C)n1nc2c(c1-c1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4791646 182837 0 None -2 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 323 2 1 3 3.8 CC(C)n1nc2c(c1-c1ccc(C(F)(F)F)cc1)CCNCC2 10.1016/j.bmcl.2020.127669
10527432 36256 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1Cl)CC2 10.1021/jm990388c
CHEMBL14458 36256 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 447 3 1 3 6.0 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1Cl)CC2 10.1021/jm990388c
10550405 38027 0 None -5 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14606 38027 0 None -5 3 Human 8.3 pKi = 8.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 427 3 1 3 5.7 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
75306277 109227 0 None -2 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109227 0 None -2 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
166 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
3045227 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
CHEMBL76781 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2003.05.001
166 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
3045227 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
CHEMBL76781 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1016/j.bmcl.2005.10.029
11536843 115097 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343673 115097 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)[C@@]1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
11500509 120555 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343670 120555 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545812 120555 0 None -3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 307 1 2 2 2.1 NC(N)=NC(=O)c1ccc2c(c1)C1(CCCO1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
31101 726 40 None -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 726 40 None -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 726 40 None -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 726 40 None -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 726 40 None -26 36 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
10331436 323 10 None -2 6 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 323 10 None -2 6 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 323 10 None -2 6 Human 8.3 pKi = 8.3 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
242 469 124 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
34 469 124 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
60795 469 124 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
CHEMBL1112 469 124 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
DB01238 469 124 None -1 52 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
44364163 39758 1 None -3 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 190 1 2 1 2.1 NC1CC1c1c[nH]c2ccc(F)cc12 10.1021/jm980318q
CHEMBL147656 39758 1 None -3 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 190 1 2 1 2.1 NC1CC1c1c[nH]c2ccc(F)cc12 10.1021/jm980318q
118464420 138220 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL3770342 138220 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acsmedchemlett.8b00300
127035063 136461 0 None 21 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
CHEMBL3736149 136461 0 None 21 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccccc1CCCN(CCc1ccc(OC)c(OC)c1)CCc1ccc2c(c1)OCO2 10.1039/C4MD00418C
44404886 72196 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL198124 72196 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL5077293 214468 0 None -17 9 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
136118648 76292 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 76292 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
118729266 120674 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402676 120674 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547137 120674 0 None 1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2cccc(Cl)c2)C1 10.1016/j.bmc.2015.01.060
10837002 35336 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1021/jm990388c
CHEMBL14374 35336 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1021/jm990388c
18475647 197689 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 334 5 2 3 4.7 CCN(CC)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
CHEMBL57135 197689 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 334 5 2 3 4.7 CCN(CC)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
10837002 35336 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL14374 35336 0 None -79 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 444 4 1 5 5.2 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298175 100913 0 None -39 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL294030 100913 0 None -39 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(Oc3cccnc3Cl)nc1)CC2 10.1016/s0960-894x(00)00364-4
11742218 195770 0 None -25 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 4 1 4 5.4 CCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55792 195770 0 None -25 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 408 4 1 4 5.4 CCc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
18931202 206780 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1ccc(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL90346 206780 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 393 7 2 5 2.4 COc1ccc(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
73350823 102503 0 None -33 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by competitive binding assayBinding affinity to human 5HT2B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 102503 0 None -33 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by competitive binding assayBinding affinity to human 5HT2B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 102503 0 None -33 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by competitive binding assayBinding affinity to human 5HT2B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
10257042 204338 0 None -12 7 Human 6.3 pKi = 6.3 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 204338 0 None -12 7 Human 6.3 pKi = 6.3 Binding
Binding affinity for 5-hydroxytryptamine 2B receptor was determinedBinding affinity for 5-hydroxytryptamine 2B receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
9866423 72275 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 413 7 0 4 4.1 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198330 72275 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 413 7 0 4 4.1 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
24887527 79997 0 None -100 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 4.9 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
CHEMBL212886 79997 0 None -100 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 4.9 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.05.034
24887290 80220 0 None -630 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL213839 80220 0 None -630 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(N2CC=C(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
44414051 166203 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 5.0 COc1ccc(C2=C(C)CN(c3ccc(Cl)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL426684 166203 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 440 7 0 4 5.0 COc1ccc(C2=C(C)CN(c3ccc(Cl)cc3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
10454231 168937 0 None -79 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(C2=CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL438963 168937 0 None -79 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 410 7 0 4 4.1 COc1ccc(C2=CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
11292933 56364 45 None -2511 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631540 56364 45 None -2511 9 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
44298100 196042 0 None -158 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2ccc(Cl)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL56050 196042 0 None -158 3 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.5 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2ccc(Cl)c3Cl)cn1 10.1016/s0960-894x(00)00364-4
153287551 169928 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 307 1 0 2 3.8 CC(=O)N1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
CHEMBL4441621 169928 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 307 1 0 2 3.8 CC(=O)N1CC[C@H]2c3cccc(-c4ccccc4)c3OC[C@]21C 10.1021/acsmedchemlett.9b00225
153287553 171080 0 None -79 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4457754 171080 0 None -79 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
17989823 152052 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.0 COc1ccc(N2Cc3cccc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL396748 152052 0 None -316 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 448 6 0 4 5.0 COc1ccc(N2Cc3cccc(C(F)(F)F)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10813396 98688 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cc(F)cc(F)c3)c1)CC2 10.1021/jm990388c
CHEMBL277732 98688 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 449 3 1 3 5.6 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cc(F)cc(F)c3)c1)CC2 10.1021/jm990388c
18357723 195497 0 None -31 3 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 424 4 1 4 4.4 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Br)ccc21 10.1016/s0960-894x(00)00365-6
CHEMBL55388 195497 0 None -31 3 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 424 4 1 4 4.4 O=C(Nc1ccc(OCc2ccccn2)nc1)N1CCc2cc(Br)ccc21 10.1016/s0960-894x(00)00365-6
44298129 195934 0 None -125 2 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 364 3 1 4 4.3 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55958 195934 0 None -125 2 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 364 3 1 4 4.3 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
2028 2958 80 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2958 80 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2958 80 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2958 80 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2958 80 None -40 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
136020617 57293 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/np100588c
CHEMBL1651095 57293 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptor by radioligand displacement assayBinding affinity to human 5HT2B receptor by radioligand displacement assay
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/np100588c
132060770 162615 0 None -8 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4169689 162615 0 None -8 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
135367820 164797 0 None -9 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 164797 0 None -9 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
135846981 93023 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1/N/C(=C/c2c[nH]c3ccccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442265 93023 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1/N/C(=C/c2c[nH]c3ccccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL5306285 194560 0 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL 486 7 2 9 3.2 C[C@H](NC(=O)c1cn(C2(C#N)CC2)cn1)C(=O)Nc1nc(-c2cccc(-c3ccn(C)n3)c2)cs1 10.6019/CHEMBL5303766
CHEMBL5072247 214252 5 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL None None None CC[C@H]1CN2CCc3c([nH]c4cccc(O)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
145980271 166468 0 None 1 16 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 166468 0 None 1 16 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4475494 213928 6 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CC(C)(O)[C@H](F)CN1Cc2cc(NC(=O)c3cnn4cccnc34)c(N3CCOCC3)cc2C1=O 10.6019/CHEMBL4879554
71452172 83489 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysis
ChEMBL 274 6 1 5 2.4 c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1 10.1021/ml3002715
CHEMBL2203551 83489 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by microbeta scintillation counting analysis
ChEMBL 274 6 1 5 2.4 c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1 10.1021/ml3002715
46230100 199296 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590531 199296 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
127049981 140574 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(I)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3813789 140574 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 573 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(I)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
135464118 93031 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442272 93031 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
155556596 174399 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of human 5HT2B by radio-ligand binding displacement assayInhibition of human 5HT2B by radio-ligand binding displacement assay
ChEMBL 428 5 4 7 3.1 OC[C@@]12C[C@@H]1[C@@H](n1cc(-c3ccccc3)c3c(Nc4ccccc4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b00689
CHEMBL4552895 174399 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of human 5HT2B by radio-ligand binding displacement assayInhibition of human 5HT2B by radio-ligand binding displacement assay
ChEMBL 428 5 4 7 3.1 OC[C@@]12C[C@@H]1[C@@H](n1cc(-c3ccccc3)c3c(Nc4ccccc4)ncnc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b00689
161 751 6 None 2 6 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 751 6 None 2 6 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 751 6 None 2 6 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
58911644 91071 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397895 91071 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
136020617 57293 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL1651095 57293 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cellsDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in baculovirus infected Sf9 cells
ChEMBL 223 2 2 4 1.6 C[C@@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4475494 213928 6 None - 1 Human 6.3 pKi = 6.3 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CC(C)(O)[C@H](F)CN1Cc2cc(NC(=O)c3cnn4cccnc34)c(N3CCOCC3)cc2C1=O 10.6019/CHEMBL4879554
44407460 140325 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
CHEMBL380763 140325 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 315 5 1 3 4.4 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCc1ccccc1 10.1016/j.bmcl.2005.10.029
90181061 160847 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
CHEMBL4115017 160847 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 381 5 0 5 2.4 Cc1ncccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
145 140 49 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
1832 140 49 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
CHEMBL7257 140 49 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
DB14010 140 49 None -87 30 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm050663x
2726 916 68 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
621 916 68 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
83 916 68 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
CHEMBL71 916 68 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
DB00477 916 68 None -19 73 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm100600y
72735042 106283 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 293 2 3 2 1.6 NC(N)=NC(=O)/C=C/c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3092763 106283 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 293 2 3 2 1.6 NC(N)=NC(=O)/C=C/c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
CHEMBL3139089 106283 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 293 2 3 2 1.6 NC(N)=NC(=O)/C=C/c1ccc2c(c1)C(O)c1ccccc1-2 10.1016/j.bmc.2013.10.010
127036953 137490 0 None -5 22 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 137490 0 None -5 22 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
118709751 113514 0 None -407 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 113514 0 None -407 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
136118653 93025 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3ccc(Br)cc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442267 93025 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3ccc(Br)cc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
54764240 68839 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922539 68839 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 242 1 1 2 2.7 CC/C=C1\C[C@H]2CNc3ccccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL4592872 213997 0 None -4 3 Human 5.3 pKi = 5.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000340a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000340a HTR2B
ChEMBL None None None O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@H]1c1ccc(F)cc1 10.6019/CHEMBL5212743
58405078 110669 0 None -6 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 310 5 1 5 3.0 Cc1nc(COc2ccc(Cl)cc2OC2CNC2)cs1 10.1021/ml500082j
CHEMBL3260335 110669 0 None -6 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 310 5 1 5 3.0 Cc1nc(COc2ccc(Cl)cc2OC2CNC2)cs1 10.1021/ml500082j
398712 77840 5 None -52 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
CHEMBL209324 77840 5 None -52 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor by radioligand binding assayBinding affinity to 5HT2B receptor by radioligand binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
9859144 67331 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 208 0 1 2 1.7 Clc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2005.05.074
CHEMBL188605 67331 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 208 0 1 2 1.7 Clc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2005.05.074
122178701 121341 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581246 121341 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 9 0 5 5.4 CCCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
122178708 121348 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC1CCCCC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
CHEMBL3581253 121348 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC1CCCCC1)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/acs.jnatprod.2c00365
2884131 166884 7 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4286420 166884 7 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 275 1 3 5 2.2 NC1=NC2(CCCCC2)NC(Nc2cccc(F)c2)=N1 10.1021/acsmedchemlett.8b00300
71655748 87796 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 359 5 1 4 4.8 CC(C)CCOc1ccc2c(c1)[C@H]1OCCC[C@H]1[C@@H](C1CCOCC1)N2 10.1021/jm400181k
CHEMBL2338343 87796 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 359 5 1 4 4.8 CC(C)CCOc1ccc2c(c1)[C@H]1OCCC[C@H]1[C@@H](C1CCOCC1)N2 10.1021/jm400181k
142601335 186397 0 None -44 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186397 0 None -44 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
134157367 153874 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 517 10 5 9 1.0 CC(=O)NCCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3983143 153874 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 517 10 5 9 1.0 CC(=O)NCCCNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
11644842 89068 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337105 89068 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365394 89068 0 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 244 1 2 2 1.9 Cc1cc(C(C)C)cc2c1C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
4098 32475 30 None -14 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32475 30 None -14 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32475 30 None -14 11 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL4557026 213984 0 None - 1 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000700a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000700a HTR2B
ChEMBL None None None C[C@H](NC(=O)Nc1cc2[nH]ncc2c(CO)n1)c1ccccn1 10.6019/CHEMBL5212743
54764241 68838 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922538 68838 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 258 1 1 3 2.3 C/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
18735313 204911 1 None -4 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL76307 204911 1 None -4 3 Human 7.3 pKi = 7.3 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 210 2 1 2 2.1 C[C@H](N)CN1CCc2ccc(Cl)cc21 10.1016/j.bmcl.2003.05.001
24826868 91053 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397877 91053 1 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2cc(Cl)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
127049979 140625 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(Cl)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
CHEMBL3814708 140625 1 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method
ChEMBL 481 12 0 5 5.8 COc1ccc(CCN(CCCc2ccc(Cl)cc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1016/j.bmcl.2016.05.079
5282379 194961 69 None 1 3 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
CHEMBL547 194961 69 None 1 3 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 nan
118729242 120659 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402661 120659 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547028 120659 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmc.2015.01.060
181743 178548 5 None -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL467094 178548 5 None -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2015.07.012
181743 178548 5 None -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 178548 5 None -275 22 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
16115511 84808 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223466 84808 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 250 1 1 2 2.0 CCc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
122178709 121349 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581254 121349 0 None -2 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 381 6 0 5 4.0 C=CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
4407909 192842 1 None 4 10 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192842 1 None 4 10 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192842 1 None 4 10 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
118055233 177244 0 None -38 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 214 0 1 2 2.0 c1cc2c3c(c1)C1(CCC1)CN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4636196 177244 0 None -38 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 214 0 1 2 2.0 c1cc2c3c(c1)C1(CCC1)CN3CCNC2 10.1016/j.bmcl.2019.126929
11448649 83404 0 None -27 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
CHEMBL219734 83404 0 None -27 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 272 1 1 3 1.7 O=C1c2c(OC(F)(F)F)cccc2C2CNCCN12 10.1021/jm0612968
29101 72195 2 None -10 2 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 298 5 2 4 1.8 CN(C)CCc1cn(C)c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL198123 72195 2 None -10 2 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 298 5 2 4 1.8 CN(C)CCc1cn(C)c2cccc(OP(=O)(O)O)c12 10.1016/j.bmcl.2005.06.104
71061709 149503 0 None -3 12 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 149503 0 None -3 12 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
11222829 91082 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cccc(C(F)(F)F)c2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397906 91082 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2cccc(C(F)(F)F)c2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
162669941 182631 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 4 8 1.8 CC(C)C(Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C(C)C 10.1016/j.bmcl.2020.127599
CHEMBL4788883 182631 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 4 8 1.8 CC(C)C(Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C(C)C 10.1016/j.bmcl.2020.127599
44404895 170785 0 None -12 3 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 292 3 2 2 3.9 Oc1cccc2[nH]cc(CCN3CCCc4ccccc43)c12 10.1016/j.bmcl.2005.06.104
CHEMBL445331 170785 0 None -12 3 Human 5.3 pKi = 5.3 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 292 3 2 2 3.9 Oc1cccc2[nH]cc(CCN3CCCc4ccccc43)c12 10.1016/j.bmcl.2005.06.104
CHEMBL4798829 214030 7 None 6 2 Human 6.3 pKi = 6.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000752a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000752a HTR2B
ChEMBL None None None c1ccc2oc(-c3csc(C4CCN(Cc5nc6ncccc6[nH]5)CC4)n3)cc2c1 10.6019/CHEMBL5212743
44582705 186972 0 None -3 13 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186972 0 None -3 13 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
3158 56237 27 None -389 20 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56237 27 None -389 20 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
122178699 121340 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581245 121340 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 7 0 5 4.6 CCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
216239 23763 118 None 2 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1200485 23763 118 None 2 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1336 23763 118 None 2 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
73213195 104432 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104432 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
11808247 18043 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 18043 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 18043 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11808247 18043 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 18043 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 18043 0 None -6 9 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44456400 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
44456400 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12802 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
49865830 16128 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.0 CC(C)NC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224032 16128 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 296 1 1 3 3.0 CC(C)NC(=O)N1OCC2CSc3ccc(F)cc3C21 10.1016/j.bmcl.2010.07.074
41305446 167228 1 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292719 167228 1 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
46914772 15409 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1215036 15409 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 368 7 0 4 4.1 FCCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
73213195 104432 0 None -1 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104432 0 None -1 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
122178700 121279 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3580670 121279 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 411 8 0 5 5.0 CCCCCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
71681899 91058 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397882 91058 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
2291 3162 58 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3162 58 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3162 58 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3162 58 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3162 58 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
44364514 121673 10 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 NC1CC1c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL358810 121673 10 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 NC1CC1c1c[nH]c2ccccc12 10.1021/jm980318q
10103618 121500 4 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@@H]1C[C@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL358522 121500 4 None -1 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@@H]1C[C@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
50878551 90716 61 None -1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90716 61 None -1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
11492300 89082 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
CHEMBL2337495 89082 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
CHEMBL2365471 89082 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 188 0 2 2 0.5 O=C1N[C@H]2CNC[C@@H]2c2ccccc21 10.1016/j.bmcl.2012.10.091
68691189 91079 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397903 91079 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 227 0 1 3 0.5 N#Cc1ccc2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
25117677 200229 0 None -23 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL597009 200229 0 None -23 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
176 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
127051844 140822 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140822 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
127051844 140822 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140822 0 None -48 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
136118620 76223 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2058419 76223 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
44397846 67615 0 None -22 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL190584 67615 0 None -22 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 202 0 1 2 1.7 Cc1cccc2c1N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
127034729 136340 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 463 12 0 6 5.1 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
CHEMBL3734894 136340 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 463 12 0 6 5.1 COc1cccc(CCCN(CCc2ccc(OC)c(OC)c2)Cc2ccc3c(c2)OCO3)c1 10.1039/C4MD00418C
127036910 136440 0 None 18 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 419 10 0 5 4.7 COc1ccc(CCN(CCc2ccc3c(c2)OCO3)Cc2ccccc2)cc1OC 10.1039/C4MD00418C
CHEMBL3735862 136440 0 None 18 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 419 10 0 5 4.7 COc1ccc(CCN(CCc2ccc3c(c2)OCO3)Cc2ccccc2)cc1OC 10.1039/C4MD00418C
136118615 93036 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442277 93036 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
657255 199061 34 None -9 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199061 34 None -9 15 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
45486824 197354 0 None -14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL569251 197354 0 None -14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 421 4 3 4 3.3 O=C1Cc2c(ccc3c2OC[C@H](CNCC2CCc4[nH]c5ccc(F)cc5c4C2)O3)N1 10.1016/j.bmcl.2009.08.050
135427931 73091 2 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 317 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(I)c21 10.1021/jm050663x
CHEMBL201132 73091 2 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 317 2 2 4 1.7 C[C@H](N)Cn1ncc2ccc(O)c(I)c21 10.1021/jm050663x
58911579 91067 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397891 91067 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
277 1289 62 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1289 62 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1289 62 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1289 62 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1289 62 None -5 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
118464420 138220 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 138220 0 None 26 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
118464421 167268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
CHEMBL4293638 167268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5HT2B (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 291 1 3 5 2.7 NC1=NC2(CCCCC2)NC(Nc2cccc(Cl)c2)=N1 10.1021/acsmedchemlett.8b00300
118706294 120509 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 311 3 3 3 1.3 COCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3310118 120509 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 311 3 3 3 1.3 COCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
CHEMBL3545470 120509 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 311 3 3 3 1.3 COCc1cccc2c1-c1ccc(C(=O)N=C(N)N)cc1C2O 10.1016/j.bmc.2014.05.027
44324142 206933 0 None -25 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 427 7 2 5 3.0 COc1cc(Cl)c(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
CHEMBL91221 206933 0 None -25 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 427 7 2 5 3.0 COc1cc(Cl)c(Cl)cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O 10.1016/S0960-894X(96)00503-3
10670191 40867 0 None -15 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 428 3 1 4 5.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cnccc3C)c1)CC2 10.1021/jm990388c
CHEMBL14864 40867 0 None -15 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 428 3 1 4 5.1 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3cnccc3C)c1)CC2 10.1021/jm990388c
135398745 2893 112 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2893 112 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2893 112 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2893 112 None -5 66 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cellsDisplacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
44298080 195947 0 None -1 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 431 4 1 5 4.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cncn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55969 195947 0 None -1 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 431 4 1 5 4.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3cncn3C)nc1)CC2 10.1016/s0960-894x(00)00365-6
191 402 98 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 402 98 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 402 98 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 402 98 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 402 98 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
118706292 120508 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 297 2 4 3 0.7 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(CO)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3310117 120508 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 297 2 4 3 0.7 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(CO)c1-2 10.1016/j.bmc.2014.05.027
CHEMBL3545469 120508 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation countingDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293-EBNA cells by liquid scintillation counting
ChEMBL 297 2 4 3 0.7 NC(N)=NC(=O)c1ccc2c(c1)C(O)c1cccc(CO)c1-2 10.1016/j.bmc.2014.05.027
127035065 136475 0 None 30 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
CHEMBL3736207 136475 0 None 30 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 477 13 0 6 5.2 COc1ccc(CCCN(CCc2ccc(OC)c(OC)c2)CCc2ccc3c(c2)OCO3)cc1 10.1039/C4MD00418C
73453 29585 24 None -9 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29585 24 None -9 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
118729258 120670 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402671 120670 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547133 120670 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 319 2 0 1 4.7 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmc.2015.01.060
127036186 137389 0 None -1 19 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 137389 0 None -1 19 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
71062829 160110 0 None 1 3 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
CHEMBL4108986 160110 0 None 1 3 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
10659364 120688 0 None -50 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@@H]1C[C@@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3402685 120688 0 None -50 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@@H]1C[C@@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3547178 120688 0 None -50 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@@H]1C[C@@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
122187376 122998 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 457 6 0 5 5.9 CCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609141 122998 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 457 6 0 5 5.9 CCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
9978683 18642 0 None -380 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
CHEMBL1277104 18642 0 None -380 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
53325861 56826 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL1643902 56826 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
53325861 56826 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
CHEMBL1643902 56826 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
117209858 184530 1 None -3 7 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 184530 1 None -3 7 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
46230047 199227 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590089 199227 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1ccc2c(c1)C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
24839550 137290 14 None 1 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752576 137290 14 None 1 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 2B (unknown origin) by competition binding assayBinding affinity to 5-HT 2B (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
45486891 196917 0 None -83 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
CHEMBL566379 196917 0 None -83 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 449 6 3 4 4.1 O=C1Cc2c(ccc3c2OC[C@H](CNCCCC2CCc4c([nH]c5ccc(F)cc45)C2)O3)N1 10.1016/j.bmcl.2009.08.050
27620 140793 13 None -269 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818994 140793 13 None -269 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
24360 203321 106 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
CHEMBL65 203321 106 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 348 1 1 6 2.1 CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccccc3nc2-1 nan
44315697 205482 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
CHEMBL80731 205482 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 254 4 1 3 2.6 CCSc1cc2c(cc1F)CCN2C[C@H](C)N 10.1016/j.bmcl.2003.05.001
3952 1875 38 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5353646 1875 38 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5443 1875 38 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
5702063 1875 38 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL1331786 1875 38 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
CHEMBL420 1875 38 None -3 12 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N nan
145967771 164763 0 None 3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4218231 164763 0 None 3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 223 2 2 4 1.6 C[C@H]1SC(c2ccccc2O)=N[C@@H]1CO 10.1021/acs.jnatprod.7b00317
57396813 71516 0 None -891 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human 5HT2BInhibition of human 5HT2B
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71516 0 None -891 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human 5HT2BInhibition of human 5HT2B
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71516 0 None -891 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human 5HT2BInhibition of human 5HT2B
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44407335 73065 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
CHEMBL201117 73065 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 321 5 1 3 4.7 C[C@@H](Cn1ccc2ccc3ncccc3c21)NCC1CCCCC1 10.1016/j.bmcl.2005.10.029
57799321 89032 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337491 89032 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2364961 89032 1 None -5 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@@H]2CNC[C@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
71462777 82936 0 None -83 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
CHEMBL2181171 82936 0 None -83 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 335 5 0 4 4.3 CCCN1CCC(COc2nc3ccccc3c3ncccc23)CC1 10.1021/jm300943r
56658156 65637 0 None 9 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccccc1CCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
CHEMBL1834256 65637 0 None 9 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from 5-HT2B after 1.5 hrs by liquid scintillation counting
ChEMBL 364 7 0 4 4.2 COc1ccccc1CCCN1CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmcl.2011.08.029
168281486 191010 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(OCCF)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5187013 191010 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 387 6 0 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(OCCF)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
11630147 91084 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 2 1 3 1.1 CCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397908 91084 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 246 2 1 3 1.1 CCOc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44298209 194568 0 None -19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL53113 194568 0 None -19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 395 3 1 5 4.5 Cc1cc2c(cc1Cl)N(C(=O)Nc1cnc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
44298225 195455 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 456 3 1 5 5.1 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(C(F)(F)F)c2c3CCO2)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL55292 195455 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 456 3 1 5 5.1 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3c2cc(C(F)(F)F)c2c3CCO2)cn1 10.1016/s0960-894x(00)00364-4
44298244 200052 0 None -79 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1cc2c(cc1Br)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL59584 200052 0 None -79 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 438 3 1 4 5.2 Cc1cc2c(cc1Br)N(C(=O)Nc1ccc(Oc3cccnc3C)nc1)CC2 10.1016/s0960-894x(00)00364-4
17989871 150301 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(C)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
CHEMBL395298 150301 0 None -50 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 462 6 0 4 5.6 COc1ccc(N2Cc3cc(Cl)c(C)c(Cl)c3C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.029
10693974 35635 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccc(F)cc3)c1)CC2 10.1021/jm990388c
CHEMBL14401 35635 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 431 3 1 3 5.5 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cncc(-c3ccc(F)cc3)c1)CC2 10.1021/jm990388c
10458193 86813 0 None -25 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cc(F)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
CHEMBL232254 86813 0 None -25 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 451 6 0 5 4.6 COc1ccc(N2Cc3c(c4cc(F)ccc4n3C)C2=O)cc1OCCN1CCC(C)CC1 10.1016/j.bmcl.2006.10.034
44568347 191627 0 None -30 15 Human 6.2 pKi = 6.2 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 191627 0 None -30 15 Human 6.2 pKi = 6.2 Binding
Antagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT2B receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
18475581 199576 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 4 4.3 Cc1nc2ccc(NC(=O)Nc3ccnc4ccccc34)cc2o1 10.1016/s0960-894x(01)00343-2
CHEMBL59266 199576 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 318 2 2 4 4.3 Cc1nc2ccc(NC(=O)Nc3ccnc4ccccc34)cc2o1 10.1016/s0960-894x(01)00343-2
24888180 79839 0 None -251 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 426 7 0 4 4.6 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL212270 79839 0 None -251 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 426 7 0 4 4.6 COc1ccc(N2CC=C(c3cccc(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
24887518 80255 0 None -794 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
CHEMBL213987 80255 0 None -794 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 460 7 0 4 5.3 COc1ccc(N2CC=C(c3ccc(Cl)c(Cl)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2006.05.034
44298091 101692 0 None -99 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 398 3 1 4 5.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL299530 101692 0 None -99 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 398 3 1 4 5.0 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(F)c(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
10476876 194953 0 None -158 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C(F)(F)F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL54610 194953 0 None -158 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 414 3 1 4 5.2 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(C(F)(F)F)ccc32)cn1 10.1016/s0960-894x(00)00364-4
44298182 194974 0 None -199 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 424 3 1 4 4.9 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)ccc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL54769 194974 0 None -199 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 424 3 1 4 4.9 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3cc(Br)ccc32)cn1 10.1016/s0960-894x(00)00364-4
10413595 161817 0 None -1995 11 Human 6.2 pKi = 6.2 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL414628 161817 0 None -1995 11 Human 6.2 pKi = 6.2 Binding
Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918647 100718 2 None -125 14 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL292759 100718 2 None -125 14 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HTCompound was tested for its binding affinity against cloned human 5-hydroxytryptamine 2B receptor in HEK 293 cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
18931344 206511 0 None -19 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 544 11 3 8 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1 10.1016/S0960-894X(96)00503-3
CHEMBL88571 206511 0 None -19 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 544 11 3 8 2.5 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccccc1 10.1016/S0960-894X(96)00503-3
155557042 174533 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 1 1 3 1.9 COc1ccc2c(c1)[C@@H]1CCN[C@]1(C)CO2 10.1021/acsmedchemlett.9b00225
CHEMBL4556297 174533 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 1 1 3 1.9 COc1ccc2c(c1)[C@@H]1CCN[C@]1(C)CO2 10.1021/acsmedchemlett.9b00225
15124 141110 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 3 2 2 2.0 CN(C)CCc1c[nH]c2cc(O)ccc12 10.1016/j.bmcl.2005.06.104
CHEMBL382750 141110 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 204 3 2 2 2.0 CN(C)CCc1c[nH]c2cc(O)ccc12 10.1016/j.bmcl.2005.06.104
118055308 177738 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 208 0 1 2 1.8 Clc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
CHEMBL4642763 177738 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 208 0 1 2 1.8 Clc1ccc2c3c1CCN3CCNC2 10.1016/j.bmcl.2019.126929
2099 9275 55 None - 1 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
CHEMBL1110 9275 55 None - 1 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O nan
25209050 181566 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 479 6 2 6 3.9 Cc1c(Cn2ncc(N3CCNCC3)cc2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL477008 181566 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 479 6 2 6 3.9 Cc1c(Cn2ncc(N3CCNCC3)cc2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
11820166 40245 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1cccc2[nH]cc(C3CC3N)c12 10.1021/jm980318q
CHEMBL148091 40245 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 202 2 2 2 2.0 COc1cccc2[nH]cc(C3CC3N)c12 10.1021/jm980318q
70695812 73255 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
CHEMBL2012686 73255 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
71062560 153404 0 None -1 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
CHEMBL3979116 153404 0 None -1 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
59511191 185499 3 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4862745 185499 3 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
44276349 99976 0 None -288 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 325 3 4 8 -0.2 CNc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
CHEMBL286739 99976 0 None -288 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 325 3 4 8 -0.2 CNc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12 10.1021/acs.jmedchem.6b01183
11427139 84658 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL222566 84658 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 282 1 1 2 2.4 C=Cc1cc2c(c(C(F)(F)F)c1)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
2274 3151 58 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3151 58 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3151 58 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3151 58 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3151 58 None -10 32 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
132060812 162012 0 None -16 10 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 162012 0 None -16 10 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
44215629 156318 1 None -12 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 206 0 1 2 1.9 N#Cc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL406585 156318 1 None -12 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 206 0 1 2 1.9 N#Cc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
118729236 120652 0 None -9 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402658 120652 0 None -9 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547011 120652 0 None -9 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2ccccc2Br)C1 10.1016/j.bmc.2015.01.060
CHEMBL4513786 213944 7 None -1174 8 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2B
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
CHEMBL4796803 213944 7 None -1174 8 Human 5.2 pKi = 5.2 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl HTR2B
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
46914776 15386 0 None 7 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214892 15386 0 None 7 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 364 7 0 4 4.5 CCCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
71062708 154282 0 None -3 12 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 154282 0 None -3 12 Mouse 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
49865886 16148 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 262 2 1 3 2.1 CCCNC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
CHEMBL1224102 16148 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 262 2 1 3 2.1 CCCNC(=O)N1OCC2COc3ccccc3C21 10.1016/j.bmcl.2010.07.074
11198145 9783 2 None -2 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL113830 9783 2 None -2 5 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
49783209 17577 0 None -114 27 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17577 0 None -114 27 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5-HT2B receptorBinding affinity to human 5-HT2B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
10539928 120681 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402668 120681 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547154 120681 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(F)cc2)C1 10.1016/j.bmc.2015.01.060
136118619 76222 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058418 76222 0 None 2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
25060119 104288 0 None -9332 7 Human 6.2 pKi = 6.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
CHEMBL3099899 104288 0 None -9332 7 Human 6.2 pKi = 6.2 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
122187377 122999 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 485 8 0 5 6.7 CCCCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609142 122999 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 485 8 0 5 6.7 CCCCCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL5071978 214249 0 None 1 6 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44397752 125243 0 None -7 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
CHEMBL364534 125243 0 None -7 3 Human 7.2 pKi = 7.2 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 216 0 1 2 2.0 Cc1ccc2c(c1C)N1[C@H](CNC[C@H]1C)C2 10.1016/j.bmcl.2005.05.074
46230097 199343 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
CHEMBL590816 199343 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
130442480 175246 0 None -83 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 175246 0 None -83 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
134150123 152066 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 4 2 9 0.4 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3967613 152066 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 381 4 2 9 0.4 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)C)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
3033538 1307 39 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
7155 1307 39 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
781 1307 39 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
CHEMBL1201216 1307 39 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
DB00298 1307 39 None -12 9 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 nan
16118795 60066 0 None -954 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642851 60066 0 None -954 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739215 60066 0 None -954 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16117153 60109 0 None -1122 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642889 60109 0 None -1122 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739616 60109 0 None -1122 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
70695812 73255 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
CHEMBL2012686 73255 0 None -831 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.6b01183
44352308 117461 0 None -83 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligandBinding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
CHEMBL339980 117461 0 None -83 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligandBinding affinity towards human 5-hydroxytryptamine 2B receptor using [3H]5-HT as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
122442272 138323 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 138323 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 138323 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
213 3824 55 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3824 55 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3824 55 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3824 55 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3824 55 None -5 44 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
44409097 76577 0 None -4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 257 0 1 3 1.8 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL206333 76577 0 None -4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 257 0 1 3 1.8 C[C@@H]1CNC[C@H]2Cc3ccc(C(F)(F)F)nc3N12 10.1016/j.bmcl.2005.11.083
44626329 197385 0 None -20 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
CHEMBL569513 197385 0 None -20 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 10.1016/j.bmcl.2009.08.050
11148641 91061 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL2397885 91061 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 216 0 1 2 1.0 C[C@H]1CN2C(=O)c3ccccc3C[C@@H]2CN1 10.1016/j.bmcl.2013.04.061
CHEMBL5091373 215544 0 None -33 9 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 215544 0 None -33 9 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2351 3261 64 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
2820 3261 64 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
5035 3261 64 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
CHEMBL81 3261 64 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
DB00481 3261 64 None -7 21 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm100600y
122442272 138323 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 138323 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 138323 0 None -2 15 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT2B receptor by radioligand binding assayBinding affinity to human 5HT2B receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
9909648 205550 3 None -22 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm100600y
CHEMBL81330 205550 3 None -22 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm100600y
145977799 163619 0 None 1 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204036 163619 0 None 1 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4778870 214024 8 None -1 5 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CC1CCN(c2ccnc(NCc3cn(C)cn3)n2)CC1 10.6019/CHEMBL4800732
12488 1644 56 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1644 56 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1644 56 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1644 56 None -11 23 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
53324553 56825 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 56825 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT2B receptor (unknown origin) by PDSP assayInhibition of 5-HT2B receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
53324553 56825 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 56825 0 None -9 10 Human 5.2 pKi = 5.2 Binding
Inhibition of 5HT2B receptorInhibition of 5HT2B receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL4778870 214024 8 None -1 5 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None CC1CCN(c2ccnc(NCc3cn(C)cn3)n2)CC1 10.6019/CHEMBL4800732
16115271 79079 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
CHEMBL2113264 79079 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 298 1 1 2 2.8 CC(C)[C@H]1CNC[C@H]2c3cccc(C(F)(F)F)c3C(=O)N12 10.1021/jm0612968
71720492 86939 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 493 8 2 5 3.0 C=CCN1C[C@H](C(=O)N(CCCN2CCOCC2)C(=O)NCC)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/ml3003814
CHEMBL2323578 86939 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
ChEMBL 493 8 2 5 3.0 C=CCN1C[C@H](C(=O)N(CCCN2CCOCC2)C(=O)NCC)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/ml3003814
135398737 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
9803032 191429 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 435 7 0 4 4.4 COc1ccccc1N1CCN(CC[C@@H](C(=O)N2CCCCCC2)c2ccccc2)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5193178 191429 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL 435 7 0 4 4.4 COc1ccccc1N1CCN(CC[C@@H](C(=O)N2CCCCCC2)c2ccccc2)CC1 10.1021/acs.jmedchem.2c00633
3649661 138194 7 None 23 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 138194 7 None 23 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
2247 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
11708275 72683 3 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
CHEMBL199775 72683 3 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 3 1 4 1.4 COc1ccc2cnn(C[C@H](C)N)c2c1 10.1021/jm050663x
134 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
1775 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
9681 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
CHEMBL1065 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
DB00247 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
134 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
1775 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
9681 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
CHEMBL1065 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
DB00247 2497 24 None -2 68 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1016/j.bmcl.2013.12.024
11949710 199879 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL594717 199879 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 355 4 1 4 3.5 Cc1ccc(F)cc1CO[C@H]1CCc2ccc(N3CCNC[C@H]3C)nc21 10.1016/j.bmcl.2009.10.112
36906 104853 75 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
CHEMBL31115 104853 75 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm050663x
36906 104853 75 None -1 5 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm030205t
CHEMBL31115 104853 75 None -1 5 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligandInhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm030205t
44573547 187608 0 None -11 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assayBinding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assay
ChEMBL 348 5 1 5 2.6 C[C@H](Cc1cccc(F)c1)Oc1nc(N2CCNC[C@H]2C)ncc1F 10.1021/acs.jmedchem.2c00633
CHEMBL494948 187608 0 None -11 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assayBinding affinity to human recombinant 5-HT2B expressed in HEK293 cells assessed as inhibition constant by radioligand binding assay
ChEMBL 348 5 1 5 2.6 C[C@H](Cc1cccc(F)c1)Oc1nc(N2CCNC[C@H]2C)ncc1F 10.1021/acs.jmedchem.2c00633
9931534 34079 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL14255 34079 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 413 3 1 3 5.4 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
10623205 99039 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 445 3 1 3 5.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(F)c(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL280465 99039 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 445 3 1 3 5.8 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(F)c(C)c(-c3cccnc3)c1)CC2 10.1021/jm990388c
10837468 162684 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 455 3 1 4 5.3 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc3c(c(-c4cccnc4)c1)OCC3)CC2 10.1021/jm990388c
CHEMBL417082 162684 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand.
ChEMBL 455 3 1 4 5.3 COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc3c(c(-c4cccnc4)c1)OCC3)CC2 10.1021/jm990388c
10622480 167012 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
CHEMBL428879 167012 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 2B receptor expressed in HEK293 cells
ChEMBL 429 3 1 3 6.1 CSc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cccc(-c3cccnc3)c1)CC2 10.1021/jm990388c
44298176 100600 0 None -6 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccncc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL291949 100600 0 None -6 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 394 4 1 4 4.6 Cc1cc2c(cc1Cl)N(C(=O)Nc1ccc(OCc3ccncc3)nc1)CC2 10.1016/s0960-894x(00)00365-6
18357730 195886 0 None -19 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(OCc3ccccn3)c(C)c1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL55914 195886 0 None -19 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 442 4 1 4 5.3 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(OCc3ccccn3)c(C)c1)CC2 10.1016/s0960-894x(00)00365-6
44453103 98033 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 296 4 1 4 2.9 CCN(CC)c1nc2c(c(-c3ccc(C)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL273173 98033 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity at 5HT2B receptorBinding affinity at 5HT2B receptor
ChEMBL 296 4 1 4 2.9 CCN(CC)c1nc2c(c(-c3ccc(C)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
240 941 43 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
2769 941 43 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
44279790 941 43 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
660 941 43 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL1729 941 43 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
CHEMBL560739 941 43 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
DB00604 941 43 None -6 25 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N nan
11737939 84198 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL220900 84198 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 2.1 O=C1c2c(ccc(Cl)c2Cl)[C@@H]2CNCCN12 10.1021/jm0612968
118729268 120675 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402677 120675 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547138 120675 0 None -22 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 269 2 0 1 3.8 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(F)c2)C1 10.1016/j.bmc.2015.01.060
118729254 120682 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402669 120682 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547155 120682 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 296 3 0 3 3.6 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc([N+](=O)[O-])c2)C1 10.1016/j.bmc.2015.01.060
16062136 157644 4 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 1 1 3 3.2 CC(C)(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
CHEMBL408155 157644 4 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 285 1 1 3 3.2 CC(C)(C)c1nc2c(c(-c3ccc(F)cc3)n1)CNCC2 10.1016/j.bmcl.2008.01.090
146159245 188426 30 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
451415 188426 30 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
86289437 188426 30 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
CHEMBL502620 188426 30 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC nan
12613159 187302 11 None -2 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL493054 187302 11 None -2 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
10517285 120686 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402683 120686 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547176 120686 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccccc2Cl)C1 10.1016/j.bmc.2015.01.060
1224 1420 83 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1420 83 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1420 83 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1420 83 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1420 83 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1420 83 None -6 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
122187381 123002 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 401 2 1 5 4.5 COc1cc2c3c(c1O)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609146 123002 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 401 2 1 5 4.5 COc1cc2c3c(c1O)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
135465870 188967 8 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL508657 188967 8 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.6 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
155565326 175561 0 None -467 7 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 462 6 5 9 0.5 O=C(NCCO)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4579650 175561 0 None -467 7 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 462 6 5 9 0.5 O=C(NCCO)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@H]4C[C@H]5CC[C@@H]4C5)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
46914620 15401 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1214962 15401 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 350 6 0 4 4.1 CCOc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
46230094 199288 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
CHEMBL590482 199288 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 237 0 2 3 0.8 O=C1NC2CNCCN2c2ccc(Cl)cc21 10.1016/j.bmcl.2009.12.014
57403525 70125 0 None -478 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 70125 0 None -478 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
127051845 140704 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140704 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
4178 195780 63 None - 1 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
CHEMBL558 195780 63 None - 1 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N nan
127051845 140704 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140704 0 None -42 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
145986752 167252 0 None -1 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 167252 0 None -1 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
11695000 89042 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2337490 89042 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
CHEMBL2365083 89042 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 256 0 2 2 1.5 O=C1N[C@H]2CNC[C@@H]2c2cccc(C(F)(F)F)c21 10.1016/j.bmcl.2012.10.091
118729276 120663 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402682 120663 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547045 120663 0 None -14 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 327 3 0 1 5.4 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmc.2015.01.060
134152157 153115 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
CHEMBL3976579 153115 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 393 6 4 8 1.4 CC[C@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CO)C[C@H]12)C1CC1 10.1021/acs.jmedchem.6b01183
21830793 91806 10 None -489 46 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91806 10 None -489 46 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
16115392 84768 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL223292 84768 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 236 0 1 2 1.7 Cc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
11665991 199321 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CNCCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
CHEMBL590721 199321 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 251 0 2 3 1.2 O=C1NC2CNCCCN2c2cccc(Cl)c21 10.1016/j.bmcl.2009.12.014
222757 99348 73 None -1 3 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
CHEMBL282575 99348 73 None -1 3 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O nan
2812 4747 101 None -40 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4747 101 None -40 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44407440 139281 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL379223 139281 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 329 5 1 3 4.7 Cc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
24740863 89129 0 None 1 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL236610 89129 0 None 1 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
46214153 110668 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
CHEMBL3260334 110668 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
11221167 84651 0 None -10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL222514 84651 0 None -10 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 256 0 1 2 1.8 O=C1c2c(cccc2C(F)(F)F)[C@@H]2CNCCN12 10.1021/jm0612968
CHEMBL4520788 213952 10 None -3 25 Human 7.1 pKi = 7.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR2BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR2B
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
155535754 172051 0 None 13 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 301 1 1 4 1.2 Cc1cccc(C)c1N1C(=O)CNC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4472251 172051 0 None 13 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 301 1 1 4 1.2 Cc1cccc(C)c1N1C(=O)CNC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
44404906 70241 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 2 2 2.4 CC(Cc1c[nH]c2cccc(O)c12)N(C)C 10.1016/j.bmcl.2005.06.104
CHEMBL194202 70241 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 3 2 2 2.4 CC(Cc1c[nH]c2cccc(O)c12)N(C)C 10.1016/j.bmcl.2005.06.104
24873261 183170 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 241 2 1 3 2.3 CCn1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
CHEMBL4795756 183170 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assayDisplacement of [3H]-ketanserin from human 5-HT2B receptor by competitive radioligand binding assay
ChEMBL 241 2 1 3 2.3 CCn1nc2c(c1-c1ccccc1)CCNCC2 10.1016/j.bmcl.2020.127669
16115644 136935 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL374436 136935 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 246 2 1 3 1.4 CCc1cc2c(cc1OC)C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
145964150 164282 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4212246 164282 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
118567543 171344 0 None -7 3 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 463 4 0 4 4.2 O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2 10.1021/acs.jmedchem.9b01256
CHEMBL4461774 171344 0 None -7 3 Human 6.1 pKi = 6.1 Binding
Inhibition of 5HT2B receptor (unknown origin)Inhibition of 5HT2B receptor (unknown origin)
ChEMBL 463 4 0 4 4.2 O=C1N(c2cccnc2C(F)(F)F)CC2(CCN(CCc3ccccc3F)CC2)OC12CC2 10.1021/acs.jmedchem.9b01256
88912137 110671 0 None -245 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 405 5 1 3 5.2 C[C@@H](Oc1ccc(C(F)(F)F)cc1OC1CNC1)c1cccc(C(F)(F)F)c1 10.1021/ml500082j
CHEMBL3260337 110671 0 None -245 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 405 5 1 3 5.2 C[C@@H](Oc1ccc(C(F)(F)F)cc1OC1CNC1)c1cccc(C(F)(F)F)c1 10.1021/ml500082j
122188580 123159 0 None -19 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 485 5 4 8 2.4 CCCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.9b00637
CHEMBL3612941 123159 0 None -19 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 485 5 4 8 2.4 CCCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.9b00637
71062889 148250 0 None -41 5 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
CHEMBL3936595 148250 0 None -41 5 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
44409096 76746 0 None -28 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 203 0 1 3 1.1 Cc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL206845 76746 0 None -28 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 203 0 1 3 1.1 Cc1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
134138769 147646 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
CHEMBL3931747 147646 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting methodDisplacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method
ChEMBL 419 6 4 8 1.7 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(N[C@@H](C4CCC4)C4CC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.6b01183
132559161 172998 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2b (unknown origin)Binding affinity to 5HT2b (unknown origin)
ChEMBL 538 7 2 7 1.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccoc2)N(C)C(=O)[C@H](Cc2ccoc2)NC(=O)[C@H](Cc2ccoc2)N(C)C1=O 10.1039/C9MD00050J
CHEMBL4518571 172998 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2b (unknown origin)Binding affinity to 5HT2b (unknown origin)
ChEMBL 538 7 2 7 1.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccoc2)N(C)C(=O)[C@H](Cc2ccoc2)NC(=O)[C@H](Cc2ccoc2)N(C)C1=O 10.1039/C9MD00050J
90181066 160139 0 None 9 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 380 5 0 4 3.1 Cc1ccccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
CHEMBL4109218 160139 0 None 9 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 380 5 0 4 3.1 Cc1ccccc1OC[C@H]1CN(CC(=O)N2c3ccccc3CC2C)CCO1 nan
136118652 93024 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cccc(Br)c23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442266 93024 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3cccc(Br)c23)C(=O)N1C 10.1016/j.bmc.2013.09.011
11673842 89059 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337498 89059 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365254 89059 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 264 2 2 2 2.1 CCCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
11361103 91076 1 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2ccc(C(F)(F)F)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397900 91076 1 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 270 0 1 2 1.7 O=C1c2ccc(C(F)(F)F)cc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
18715554 74395 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL202656 74395 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 225 2 1 3 2.5 C[C@H](N)Cn1ccc2ccc3cnccc3c21 10.1016/j.bmcl.2005.10.029
24826871 91083 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397907 91083 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
25122653 200504 0 None -17 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL598850 200504 0 None -17 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
136118638 76287 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058698 76287 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
136118730 76215 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
CHEMBL2058407 76215 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2cccc(Br)c12 10.1016/j.bmc.2013.09.011
71062567 160391 0 None 2 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111349 160391 0 None 2 2 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
54764239 68837 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
CHEMBL1922537 68837 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 minsInhibition of human 5HT2B receptor expressed in cos-7 cells assessed as [3H]5-HT uptake after 120 mins
ChEMBL 272 2 1 3 2.7 CC/C=C1\C[C@H]2CNc3c(OC)cccc3C(=O)N2C1 10.1016/j.bmcl.2011.09.086
11630623 89070 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337499 89070 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365399 89070 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1ccc(Cl)c2c1[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
56649649 67828 0 None -93 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910140 67828 0 None -93 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
86221574 166663 2 None 9 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
CHEMBL4282117 166663 2 None 9 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
162674022 183197 0 None - 1 Human 7.1 pKi = 7.1 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
CHEMBL4796102 183197 0 None - 1 Human 7.1 pKi = 7.1 Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assayAntagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
ChEMBL 305 4 1 4 3.5 N#Cc1cccc(CCCc2cc(=O)c3c(O)cccc3o2)c1 10.1016/j.bmcl.2020.127511
44299663 163102 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 306 3 2 3 3.9 CN(C)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
CHEMBL417753 163102 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 2B receptorBinding affinity against 5-hydroxytryptamine 2B receptor
ChEMBL 306 3 2 3 3.9 CN(C)c1ccc(NC(=O)Nc2ccnc3ccccc23)cc1 10.1016/s0960-894x(01)00343-2
10127939 72213 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 477 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
CHEMBL198171 72213 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 477 7 0 4 5.3 COc1ccc(N2CCN(c3ccc(C)c(C(F)(F)F)c3)C2=O)cc1OCCN1CCCCC1 10.1016/j.bmcl.2005.08.004
49850772 56369 0 None -501 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 397 5 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc(-n5cccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631545 56369 0 None -501 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 397 5 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc(-n5cccn5)c4)CC3)cccc2n1 10.1021/jm100714c
44298208 194663 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cn1)CC2 10.1016/s0960-894x(00)00364-4
CHEMBL53308 194663 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 429 3 1 5 4.9 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cn1)CC2 10.1016/s0960-894x(00)00364-4
18931357 206565 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/S0960-894X(96)00503-3
CHEMBL88894 206565 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cellsDisplacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells
ChEMBL 578 11 3 8 3.2 COc1cc(OC)c(C(=O)CCCCN2CCC3(CC2)NC(=O)NC3=O)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/S0960-894X(96)00503-3
153287568 170961 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 217 0 1 2 2.5 Cc1cc(C)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
CHEMBL4456195 170961 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 217 0 1 2 2.5 Cc1cc(C)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
12017598 168093 0 None -15 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nn1)CC2 10.1016/s0960-894x(00)00365-6
CHEMBL432879 168093 0 None -15 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.In vitro binding affinity at human cloned 5-hydroxytryptamine 2B receptor of HEK293 cells by [3H]5-HT displacement.
ChEMBL 429 4 1 5 4.4 Cc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1ccc(OCc3ccccn3)nn1)CC2 10.1016/s0960-894x(00)00365-6
21533446 70126 0 None -213 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 70126 0 None -213 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
117209964 186110 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4871980 186110 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
10194524 72523 0 None -63 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 415 7 0 5 3.0 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
CHEMBL199177 72523 0 None -63 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HTBinding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT
ChEMBL 415 7 0 5 3.0 COc1ccc(N2CCN(c3cccc(F)c3)C2=O)cc1OCCN1CCOCC1 10.1016/j.bmcl.2005.08.004
49850567 56439 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632217 56439 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT2B receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT2B receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
44298142 101718 0 None -199 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
CHEMBL299726 101718 0 None -199 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HTBinding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT
ChEMBL 380 3 1 4 4.8 Cc1ncccc1Oc1ccc(NC(=O)N2CCc3ccc(Cl)cc32)cn1 10.1016/s0960-894x(00)00364-4
153287574 175223 0 None -10 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 175223 0 None -10 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor stably expressed in HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10368126 86690 0 None -25 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 449 7 0 6 4.2 COc1ccc2c(c1)c1c(n2C)CN(c2ccc(OC)c(OCCN3CCCCC3)c2)C1=O 10.1016/j.bmcl.2006.10.034
CHEMBL231833 86690 0 None -25 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293 cells
ChEMBL 449 7 0 6 4.2 COc1ccc2c(c1)c1c(n2C)CN(c2ccc(OC)c(OCCN3CCCCC3)c2)C1=O 10.1016/j.bmcl.2006.10.034
25164129 161136 0 None -1479 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4088036 161136 0 None -1479 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117406 161136 0 None -1479 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25056080 65660 0 None -407 2 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834345 65660 0 None -407 2 Human 5.1 pKi = 5.1 Binding
Inhibition of human 5-HT2B receptorInhibition of human 5-HT2B receptor
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
24826788 91069 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397893 91069 0 None 7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 236 0 1 2 1.3 O=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
71657836 120671 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402673 120671 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547134 120671 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 329 2 0 1 4.5 CN(C)[C@@H]1Cc2ccccc2[C@@H](c2cccc(Br)c2)C1 10.1016/j.bmc.2015.01.060
135453290 133581 33 None -2 8 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133581 33 None -2 8 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
134551 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
30241 42014 16 None -8 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 204 3 2 2 2.2 COc1ccc2[nH]cc(C(C)CN)c2c1 10.1021/jm980318q
CHEMBL149564 42014 16 None -8 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 204 3 2 2 2.2 COc1ccc2[nH]cc(C(C)CN)c2c1 10.1021/jm980318q
11492162 72024 3 None 10 4 Human 8.1 pKi = 8.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197646 72024 3 None 10 4 Human 8.1 pKi = 8.1 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 206 3 1 1 2.4 CN(C)CCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2005.06.104
11615459 199225 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
CHEMBL590078 199225 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cellsDisplacement of [125I]LSD from human recombinant 5HT2B receptor expressed in HEK293E cells
ChEMBL 217 0 2 3 0.5 Cc1cccc2c1C(=O)NC1CNCCN21 10.1016/j.bmcl.2009.12.014
135414348 72780 2 None -4 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
CHEMBL200104 72780 2 None -4 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells
ChEMBL 205 2 2 4 1.4 Cc1c(O)ccc2cnn(C[C@H](C)N)c12 10.1021/jm050663x
CHEMBL5082177 214769 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT2BR (unknown origin)Binding affinity to 5-HT2BR (unknown origin)
ChEMBL None None None CCCN(CCC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2726 916 68 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 916 68 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 916 68 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 916 68 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 916 68 None -19 73 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
122178698 121339 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL3581244 121339 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 369 5 0 5 3.9 CCOc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
10827035 120679 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3402666 120679 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
CHEMBL3547152 120679 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 285 2 0 1 4.3 CN(C)[C@H]1Cc2ccccc2[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.01.060
118729281 120658 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@H]1C[C@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3402686 120658 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@H]1C[C@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
CHEMBL3547018 120658 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 265 2 0 1 4.0 Cc1ccccc1[C@H]1C[C@H](N(C)C)Cc2ccccc21 10.1016/j.bmc.2015.01.060
44409316 74992 0 None -102 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@H]2Cc3ccc(Br)nc3N12 10.1016/j.bmcl.2005.11.083
CHEMBL203393 74992 0 None -102 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 267 0 1 3 1.6 C[C@@H]1CNC[C@H]2Cc3ccc(Br)nc3N12 10.1016/j.bmcl.2005.11.083
145965940 164174 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 2 2 4 2.8 C[C@@H]1SC(c2cc3ccccc3cc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4210787 164174 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 2 2 4 2.8 C[C@@H]1SC(c2cc3ccccc3cc2O)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
100 3776 58 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3776 58 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3776 58 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3776 58 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3776 58 None -11 56 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
168277348 190275 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5175973 190275 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 425 8 0 5 5.4 CCCCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
155558726 174784 0 None -19 4 Human 5.1 pKi = 5.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
CHEMBL4562303 174784 0 None -19 4 Human 5.1 pKi = 5.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 835 11 0 13 6.7 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CC[C@H]3O[C@H](Cn4cc(nn4)COC[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12)[C@@H]1OC(C)(C)O[C@@H]1[C@H]3OCCC(C)C 10.1016/j.ejmech.2019.04.064
3042 1402 35 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1402 35 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1402 35 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1402 35 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1402 35 None -39 15 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
122483275 138085 0 None -3 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764133 138085 0 None -3 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765875 138085 0 None -3 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
11949706 200032 0 None -11 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
CHEMBL595645 200032 0 None -11 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]DOI from human 5HT2B receptor expressed in CHO cellsDisplacement of [125I]DOI from human 5HT2B receptor expressed in CHO cells
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
3037629 184548 18 None 1 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
CHEMBL4848517 184548 18 None 1 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to controlDisplacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control
ChEMBL 396 5 1 5 3.6 C=C[C@H]1CN2CCc3c([nH]c4cccc(OC)c34)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.1c00726
130442572 171884 0 None -17 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171884 0 None -17 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT2B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
5591 157507 90 None 1 2 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
CHEMBL408 157507 90 None 1 2 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 nan
21044398 141059 0 None -21 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 1 2 4 0.9 C[C@H](O)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
CHEMBL382618 141059 0 None -21 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 233 1 2 4 0.9 C[C@H](O)c1ccc2c(n1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.11.083
46945446 17730 0 None -5 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT2B receptorInhibition of 5-HT2B receptor
ChEMBL 408 9 0 5 4.6 CCCCOc1ccc(-c2nn3c(C)cc(C)nc3c2CC(=O)N(CC)CC)cc1 10.1016/j.bmcl.2010.07.135
CHEMBL1258723 17730 0 None -5 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT2B receptorInhibition of 5-HT2B receptor
ChEMBL 408 9 0 5 4.6 CCCCOc1ccc(-c2nn3c(C)cc(C)nc3c2CC(=O)N(CC)CC)cc1 10.1016/j.bmcl.2010.07.135
136118657 93027 0 None 12 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3c(Br)cccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2442269 93027 0 None 12 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1/N/C(=C/c2c[nH]c3c(Br)cccc23)C(=O)N1C 10.1016/j.bmc.2013.09.011
44451393 156648 1 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 211 1 1 2 2.0 COc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
CHEMBL406957 156648 1 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 211 1 1 2 2.0 COc1ccc2c(c1Cl)CCNCC2 10.1016/j.bmc.2007.12.009
11437171 83461 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
CHEMBL220207 83461 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 234 1 1 3 1.5 CSc1cccc2c1C(=O)N1CCNCC21 10.1021/jm0612968
155558968 174794 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 432 3 2 5 3.2 Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4562437 174794 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
ChEMBL 432 3 2 5 3.2 Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
44572802 12412 2 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL1186019 12412 2 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
CHEMBL445747 12412 2 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 161 2 1 1 2.1 Cc1cccc([C@H]2C[C@@H]2CN)c1 10.1021/jm801354e
136016509 136118731 10929 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
CHEMBL1173331 10929 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccc(Br)cc12 10.1016/j.bmc.2013.09.011
3168 9230 92 None -107 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9230 92 None -107 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
71450550 83778 0 None -1 16 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83778 0 None -1 16 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptorBinding affinity to 5-HT2B receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
1971 2846 38 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2846 38 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2846 38 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2846 38 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2846 38 None -4 30 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
11300712 141661 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
CHEMBL385577 141661 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1c(Cl)ccc2c1C(=O)N1CCNC[C@@H]21 10.1021/jm0612968
59757162 106277 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)-c1ccccc1C2O 10.1016/j.bmc.2013.10.010
CHEMBL3092761 106277 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)-c1ccccc1C2O 10.1016/j.bmc.2013.10.010
CHEMBL3139074 106277 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
ChEMBL 267 1 3 2 1.2 NC(N)=NC(=O)c1ccc2c(c1)-c1ccccc1C2O 10.1016/j.bmc.2013.10.010
1548953 207656 27 None -4 17 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207656 27 None -4 17 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
5870 31630 92 None - 1 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
CHEMBL1405 31630 92 None - 1 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O nan
6452095 40673 18 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 174 2 2 1 2.2 CC(CN)c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL148463 40673 18 None -9 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 174 2 2 1 2.2 CC(CN)c1c[nH]c2ccccc12 10.1021/jm980318q
11493484 89041 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337106 89041 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365079 89041 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 284 1 2 2 2.1 CCc1cc2c(c(C(F)(F)F)c1)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
21509921 104431 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104431 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
44554395 18691 0 None -54 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18691 0 None -54 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
21509921 104431 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104431 0 None -8 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)Displacement of [3H]LSD from 5-HT2B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
155565189 175541 0 None -6 4 Human 6.1 pKi = 6.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
CHEMBL4579120 175541 0 None -6 4 Human 6.1 pKi = 6.1 Binding
Antagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assayAntagonist activity at human recombinant 5-HT2B receptor in CHOK1 cells measured after 30 mins by HTRF assay
ChEMBL 634 7 0 9 6.2 CC(C)CCO[C@H]1[C@H]2CCN(CCc3ccc4ccccc4c3)CCCCCCOCc3cn(nn3)C[C@@H](O2)[C@@H]2OC(C)(C)O[C@H]12 10.1016/j.ejmech.2019.04.064
18735309 205410 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
CHEMBL80246 205410 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 262 2 1 2 2.6 C[C@H](N)CN1CCc2cc(F)c(C(F)(F)F)cc21 10.1016/j.bmcl.2003.05.001
53381002 65435 0 None 15 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
CHEMBL1829959 65435 0 None 15 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT2B receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
56649650 67829 0 None -100 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910141 67829 0 None -100 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
71062530 160068 0 None -3 2 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
CHEMBL4108620 160068 0 None -3 2 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
44407327 141222 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
CHEMBL383042 141222 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human 5HT2BDisplacement of [3H]5-HT from human 5HT2B
ChEMBL 345 6 1 4 4.4 COc1ccccc1CN[C@@H](C)Cn1ccc2ccc3ncccc3c21 10.1016/j.bmcl.2005.10.029
136118617 76220 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058416 76220 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
44315993 172853 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
CHEMBL451543 172853 0 None -15 3 Human 7.1 pKi = 7.1 Binding
Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell lineAffinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line
ChEMBL 222 3 1 3 2.1 CSc1ccc2c(c1)N(C[C@H](C)N)CC2 10.1016/j.bmcl.2003.05.001
44572810 12623 2 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL1187196 12623 2 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
CHEMBL493130 12623 2 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT2B receptorDisplacement of [3H]LSD from human 5HT2B receptor
ChEMBL 165 2 1 1 1.9 NC[C@H]1C[C@@H]1c1ccc(F)cc1 10.1021/jm801354e
11346775 83452 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL220157 83452 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cellsDisplacement of [3H]LSD from human recombinant 5HT2B expressed in HEK293E cells
ChEMBL 252 1 1 3 1.4 COc1cc(Cl)c2c(c1)[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL5094181 215457 22 None -2 5 Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None O=C(NCCCn1ccnc1)c1cc2nc(-c3ccccc3)cc(-c3ccccc3)n2n1 10.6019/CHEMBL5058647
132060776 162378 0 None -3 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 162378 0 None -3 16 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT2B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
136118658 76225 0 None 2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058426 76225 0 None 2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL5094181 215457 22 None -2 5 Human 6.1 pKi = 6.1 Binding
GPCRScan assay: inhibition of 5-HT2BGPCRScan assay: inhibition of 5-HT2B
ChEMBL None None None O=C(NCCCn1ccnc1)c1cc2nc(-c3ccccc3)cc(-c3ccccc3)n2n1 10.6019/CHEMBL5058647
13091356 113511 0 None -218 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321789 113511 0 None -218 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation countingDisplacement of [3H]LSD from human 5-HT2B receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
118717223 120556 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3343671 120556 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
CHEMBL3545813 120556 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cellsDisplacement of [3H]mesulergine from human 5-HT2B receptor expressed in HEK293 cells
ChEMBL 321 1 2 2 2.2 NC(N)=NC(=O)c1ccc2c(c1)C1(CCOCC1)c1ccccc1-2 10.1016/j.bmc.2014.09.005
46914485 15400 0 None 83 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
CHEMBL1214961 15400 0 None 83 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 336 5 0 4 3.8 COc1ccccc1CN1CCN(Cc2cc3ccccc3o2)CC1 10.1021/jm100639f
44397731 67188 0 None -23 3 Human 7.1 pKi = 7.1 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 213 0 1 3 1.3 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)cc3N12 10.1016/j.bmcl.2005.05.074
CHEMBL187888 67188 0 None -23 3 Human 7.1 pKi = 7.1 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 213 0 1 3 1.3 C[C@@H]1CNC[C@H]2Cc3ccc(C#N)cc3N12 10.1016/j.bmcl.2005.05.074
6319 23443 95 None - 1 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
CHEMBL1333512 23443 95 None - 1 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 4 2 2 5.2 c1ccc(Nc2ccc(Nc3ccccc3)cc2)cc1 nan
44451369 96305 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2c3c(ccc2o1)CCNCC3 10.1016/j.bmc.2007.12.009
CHEMBL261489 96305 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cellsDisplacement of [3H]5-HT from human 5HT2B receptor expressed in HEK293-EBNA cells
ChEMBL 187 0 1 2 2.1 c1cc2c3c(ccc2o1)CCNCC3 10.1016/j.bmc.2007.12.009
135753056 191151 2 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
CHEMBL5188949 191151 2 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) assessed as displacement of radioligand at 10 uM by radioligand binding assay
ChEMBL 337 4 2 5 2.4 CCc1cc(=O)[nH]c(-n2nc(C)cc2NC(=O)c2cccc(C)c2)n1 10.1021/acs.jmedchem.1c01759
16062145 97630 0 None -223 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 269 2 1 3 2.8 Fc1ccc(-c2nc(C3CC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
CHEMBL271111 97630 0 None -223 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cellsDisplacement of [3H]mesulergine from human recombinant 5HT2B receptor expressed in CHO cells
ChEMBL 269 2 1 3 2.8 Fc1ccc(-c2nc(C3CC3)nc3c2CNCC3)cc1 10.1016/j.bmcl.2008.01.090
11716185 89035 0 None -20 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337497 89035 0 None -20 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2364998 89035 0 None -20 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by scintillation counting analysis
ChEMBL 250 1 2 2 1.7 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
10028436 3506 5 None -45 12 Human 7.0 pKi = 7.0 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3506 5 None -45 12 Human 7.0 pKi = 7.0 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3506 5 None -45 12 Human 7.0 pKi = 7.0 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
25209705 181036 28 None -144 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 510 7 2 8 3.3 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)cc4=O)c3C)cc2)cn1 10.1021/jm800962k
CHEMBL475965 181036 28 None -144 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 510 7 2 8 3.3 COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)cc4=O)c3C)cc2)cn1 10.1021/jm800962k
168294400 192456 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC)-c1c(OC)c(OC3CCCCC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
CHEMBL5208882 192456 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 423 5 0 5 5.2 COc1cc2c(cc1OC)-c1c(OC)c(OC3CCCCC3)cc3c1[C@H](C2)N(C)CC3 10.1021/acs.jnatprod.2c00365
118055296 177927 0 None -58 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 264 2 1 2 2.7 c1ccc(Cc2ccc3c4c2CCN4CCNC3)cc1 10.1016/j.bmcl.2019.126929
CHEMBL4645736 177927 0 None -58 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)
ChEMBL 264 2 1 2 2.7 c1ccc(Cc2ccc3c4c2CCN4CCNC3)cc1 10.1016/j.bmcl.2019.126929
122483281 138083 0 None -18 8 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763779 138083 0 None -18 8 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765873 138083 0 None -18 8 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT2B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
136118649 76293 0 None 2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058704 76293 0 None 2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
11819486 121123 0 None -4 4 Human 7.0 pKi = 7.0 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@H]1C[C@@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
CHEMBL357702 121123 0 None -4 4 Human 7.0 pKi = 7.0 Binding
Binding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligandBinding affinity against the cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand
ChEMBL 172 1 2 1 2.0 N[C@H]1C[C@@H]1c1c[nH]c2ccccc12 10.1021/jm980318q
58911668 91081 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397905 91081 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysisDisplacement of [125I]LSD from human recombinant 5-HT2B receptor expressed in HEK293E cells after 45 mins by Top counting analysis
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
162652711 180356 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 3 7 2.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CF)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
CHEMBL4751718 180356 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT2B (unknown origin)Binding affinity to 5HT2B (unknown origin)
ChEMBL 409 6 3 7 2.6 CC(C)[C@@H](Nc1nc(Cl)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(CF)C[C@H]12)C1CC1 10.1016/j.bmcl.2020.127599
71452341 83668 7 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 376 6 0 3 5.3 Cc1c(C(=O)N(CCCN2CCCCC2)c2ccccc2)oc2ccccc12 10.1016/j.bmc.2012.09.044
CHEMBL2205361 83668 7 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT2B receptor after 1.5 hrs by scintillation counting analysis
ChEMBL 376 6 0 3 5.3 Cc1c(C(=O)N(CCCN2CCCCC2)c2ccccc2)oc2ccccc12 10.1016/j.bmc.2012.09.044
11848625 5760 0 None 2 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
CHEMBL1078745 5760 0 None 2 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B receptorBinding affinity to human 5HT2B receptor
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
136118614 93035 0 None 13 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442276 93035 0 None 13 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
10106214 2091 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
1207 2091 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
1209 2091 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
CHEMBL127307 2091 1 None -46 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 10.1016/j.bmc.2015.01.060
6604117 187823 6 None 1 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL2062340 187823 6 None 1 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
CHEMBL49623 187823 6 None 1 6 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assayBinding affinity to 5-HT2B receptor (unknown origin) incubated for 1 hr by radioligand binding assay
ChEMBL 325 5 2 3 3.8 C[C@@H]([C@H](O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.0c01912
49864027 15385 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 400 8 0 4 4.8 FC(F)CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
CHEMBL1214891 15385 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT2BBinding affinity to 5HT2B
ChEMBL 400 8 0 4 4.8 FC(F)CCOc1ccc(CN2CCN(Cc3cc4ccccc4o3)CC2)cc1 10.1021/jm100639f
168279369 191109 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
CHEMBL5188171 191109 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting methodDisplacement of [3H]LSD from 5-HT2B receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
ChEMBL 397 6 0 5 4.6 CCC(C)Oc1cc2c3c(c1OC)-c1cc(OC)c(OC)cc1C[C@@H]3N(C)CC2 10.1021/acs.jnatprod.2c00365
122186880 122954 0 None 4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608450 122954 0 None 4 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT2B receptor (unknown origin)Displacement of [3H]LSD from 5HT2B receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
44554227 18718 0 None -33 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277837 18718 0 None -33 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
20824949 67166 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 245 1 2 3 1.4 CC(=O)Nc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
CHEMBL187787 67166 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
ChEMBL 245 1 2 3 1.4 CC(=O)Nc1ccc2c(c1)N1[C@H](C)CNC[C@H]1C2 10.1016/j.bmcl.2005.05.074
667590 67765 12 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909048 67765 12 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 3 0 1 4.4 O=C(c1ccccc1Cl)N1CCC(Cc2ccccc2)CC1 nan
44582676 189755 0 None -7 17 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189755 0 None -7 17 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experimentInhibition of human cloned 5HT2B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
135511529 135555540 10956 0 None 5 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccccc12 10.1016/j.bmc.2013.09.011
CHEMBL1173525 10956 0 None 5 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 240 1 3 2 1.5 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2ccccc12 10.1016/j.bmc.2013.09.011
136118661 76228 0 None 6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058429 76228 0 None 6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
44112 121264 48 None -11 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 121264 48 None -11 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
124247485 164045 8 None 1 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 164045 8 None 1 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
155563428 175262 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4572905 175262 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Inhibition of 5HT2B (unknown origin)Inhibition of 5HT2B (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
44581974 175680 0 None -1 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458220 175680 0 None -1 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cellsDisplacement of [3H]5HT from 5HT2B receptor expressed in HEK293 cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
25123013 200435 0 None -27 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598443 200435 0 None -27 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation countingDisplacement of [3H]5HT from human 5HT2B receptor expressed in CHO cells by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
10383646 18730 0 None -512 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277917 18730 0 None -512 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
71450247 82947 0 None -19 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181188 82947 0 None -19 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT2B by Cerep protocol based assayBinding affinity to human 5HT2B by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
44404905 72351 1 None 3 3 Human 7.0 pKi = 7.0 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 4 2 2 2.4 CN(C)CCCc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL198617 72351 1 None 3 3 Human 7.0 pKi = 7.0 Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSOInhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD as radioligand with the compound (10 uM) dissolved in DMSO
ChEMBL 218 4 2 2 2.4 CN(C)CCCc1c[nH]c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
17683252 67767 3 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
CHEMBL1909051 67767 3 None - 1 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 347 3 0 1 4.8 O=C(c1ccccc1C(F)(F)F)N1CCC(Cc2ccccc2)CC1 nan
142601328 184979 0 None -63 5 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 184979 0 None -63 5 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
142601341 185348 0 None -3 3 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4860503 185348 0 None -3 3 Human 6.0 pKi = 6 Binding
Binding affinity to 5HT2B receptor (unknown origin)Binding affinity to 5HT2B receptor (unknown origin)
ChEMBL 272 3 2 4 1.9 COc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
56649648 67826 0 None -301 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910139 67826 0 None -301 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]LSD from 5HT2B receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
136118616 76219 0 None 3 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058415 76219 0 None 3 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
136118646 76290 0 None 2 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058701 76290 0 None 2 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT2B receptor stably expressed in HEK cells
ChEMBL 335 1 2 3 3.1 CSC1=NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
3007 155661 27 None -1 6 Rat 8.3 pKd = 8.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
Drug Central 135 2 1 1 1.6 CC(N)Cc1ccccc1 None
CHEMBL405 155661 27 None -1 6 Rat 8.3 pKd = 8.3 Binding
Affinity against serotonergic receptor in the isolated rat stomach fundusAffinity against serotonergic receptor in the isolated rat stomach fundus
Drug Central 135 2 1 1 1.6 CC(N)Cc1ccccc1 None
10615 570 32 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
46200932 570 32 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
CHEMBL4297183 570 32 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
DB14823 570 32 None 501 4 Human 11.6 pKd = 11.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
136 3267 32 None -8 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
223 3267 32 None -8 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
643606 3267 32 None -8 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
CHEMBL10347 3267 32 None -8 16 Human 8.4 pKd None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
134 2497 24 3H- LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2497 24 3H-LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H- LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H- LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H- LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H- LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-LSD -2 68 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
188 3366 80 3H-5HT -1 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
196968 3366 80 3H-5HT -1 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
CHEMBL473186 3366 80 3H-5HT -1 6 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
242 469 124 3H-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 469 124 [3H]-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 3H-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 [3H]-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 3H-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 [3H]-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 3H-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 [3H]-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 3H-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 [3H]-LSD -1 52 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2497 24 3H-5HT -2 68 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -2 68 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -2 68 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -2 68 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -2 68 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
5074 3307 80 3H-RAUWOLSCINE -2 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-RAUWOLSCINE -2 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-RAUWOLSCINE -2 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-RAUWOLSCINE -2 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
None 216026 0 3H-5HT -2 8 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
None 216026 0 3H-5HT -2 8 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
107 141 121 3H-5HT -4 31 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -4 31 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -4 31 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
None 216354 0 3H-MESULERGINE 5 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
4106 2485 22 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2485 22 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2485 22 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2485 22 3H-RAUWOLSCINE -3 34 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
134 2497 24 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-RAUWOLSCINE -2 68 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
133 2479 52 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2479 52 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2479 52 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2479 52 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2479 52 3H-MESULERGINE -2 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
133 2479 52 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2479 52 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2479 52 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2479 52 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2479 52 3H-5HT -2 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
6437377 215929 0 3H-RAUWOLSCINE 5 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
5 139 72 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2470 3626 50 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-KETANSERIN -23 60 Bovine 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 216026 0 Functional -2 8 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
1342 36 49 3H-RAUWOLSCINE 2 19 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 49 3H-RAUWOLSCINE 2 19 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 49 3H-RAUWOLSCINE 2 19 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
None 216354 0 Functional 5 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
1621 2413 17 3H-5HT -19 45 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2413 17 3H-5HT -19 45 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2413 17 3H-5HT -19 45 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2413 17 3H-5HT -19 45 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2413 17 3H-5HT -19 45 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5 139 72 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 Functional -13 55 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5074 3307 80 3H-5HT -2 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -2 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -2 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -2 30 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1588 2311 27 3H-5HT -6 44 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2311 27 3H-5HT -6 44 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2311 27 3H-5HT -6 44 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2311 27 3H-5HT -6 44 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2311 27 3H-5HT -6 44 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
188 3366 80 3H-5HT -1 6 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
196968 3366 80 3H-5HT -1 6 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
CHEMBL473186 3366 80 3H-5HT -1 6 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
None 216423 0 Functional 1 28 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
5 139 72 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 216315 0 3H-MESULERGINE -1 19 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
103 4122 61 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4122 61 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4122 61 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4122 61 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4122 61 3H-LSD 1 54 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5074 3307 80 3H-MESULERGINE -2 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-MESULERGINE -2 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-MESULERGINE -2 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-MESULERGINE -2 30 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
189 3466 39 UNDEFINED 2 17 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3466 39 UNDEFINED 2 17 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3466 39 UNDEFINED 2 17 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
11954224 215928 0 3H-5HT -66 60 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1588 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1588 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2311 27 3H-MESULERGINE -6 44 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2435 3563 83 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3563 83 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3563 83 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3563 83 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3563 83 3H-LSD -2 49 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
11957541 1446 40 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 Functional -2 16 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
206 2476 16 3H-5HT -1 25 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-5HT -1 25 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-5HT -1 25 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
134 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
6437377 215929 0 3H-5HT 5 5 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
277 1289 62 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1289 62 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1289 62 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1289 62 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1289 62 3H-5HT -5 46 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4106 2485 22 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2485 22 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2485 22 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2485 22 3H-5HT -3 34 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
135 2515 43 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -3 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
134 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
6437377 215929 0 3H-5HT 5 5 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
5074 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
134 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -2 68 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
5074 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -2 30 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
133 2479 52 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2479 52 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2479 52 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2479 52 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2479 52 3H-5HT -2 43 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 215928 0 3H- LSD -66 60 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 215928 0 3H-LSD -66 60 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
206 2476 16 3H-RAUWOLSCINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-RAUWOLSCINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-RAUWOLSCINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2476 16 3H-MESULERGINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-MESULERGINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-MESULERGINE -1 25 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
199 391 0 3H-5HT 1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
9821951 391 0 3H-5HT 1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
CHEMBL160293 391 0 3H-5HT 1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
5 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135398737 955 93 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-5HT -2 92 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
152 363 29 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 363 29 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 363 29 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
152 363 29 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 363 29 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 363 29 3H-5HT -1 19 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
7153 97992 77 3H-RAUWOLSCINE -1 34 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-RAUWOLSCINE -1 34 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
199 391 0 3H-5HT -5 5 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
9821951 391 0 3H-5HT -5 5 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
CHEMBL160293 391 0 3H-5HT -5 5 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
11957541 1446 40 3H-KETANSERIN -16 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-KETANSERIN -16 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-KETANSERIN -16 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-KETANSERIN -16 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-KETANSERIN -16 16 Bovine 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1614 203632 24 Functional 2 10 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 203632 24 Functional 2 10 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
24840389 115187 4 3H-MESULERGINE -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 115187 4 3H-MESULERGINE -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
1809 134 32 3H-KETANSERIN -109647 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-KETANSERIN -109647 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-KETANSERIN -109647 37 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1209 1645 75 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1645 75 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1645 75 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1645 75 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1645 75 3H-5HT -199 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
1357 2468 139 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2468 139 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2468 139 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2468 139 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2468 139 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2468 139 3H-5HT -3890 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
13139 2474 29 3H-KETANSERIN -66 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN None
4076 2474 29 3H-KETANSERIN -66 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN None
CHEMBL26687 2474 29 3H-KETANSERIN -66 8 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 5 1 4 1.2 COC1=CC(=CC(=C1OC)OC)CCN None
107992 2536 49 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2536 49 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2536 49 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2536 49 3H-5HT -5 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
208 2843 0 3H-5HT -69 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2843 0 3H-5HT -69 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2843 0 3H-5HT -69 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
119570 3137 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570 3137 96 3H-MESULERGINE -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3137 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3137 96 3H-MESULERGINE -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3137 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3137 96 3H-MESULERGINE -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3137 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3137 96 3H-MESULERGINE -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3137 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3137 96 3H-MESULERGINE -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
243 3180 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3180 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3180 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3180 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3180 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
2 3237 23 3H-MESULERGINE -363 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3237 23 3H-MESULERGINE -363 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3237 23 3H-MESULERGINE -363 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
128563 3438 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3438 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3438 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3438 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
2470 3626 50 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -120226 60 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2543 3681 68 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3681 68 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3681 68 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3681 68 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3681 68 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3681 68 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3681 68 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3681 68 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3681 68 3H-5HT -2818 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3681 68 3H-5HT -2818 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
46882133 5776 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
CHEMBL1078896 5776 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
46882180 5809 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
CHEMBL1079180 5809 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
2662 11352 131 3H-LSD -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11352 131 3H-LSD -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10836 14435 14 3H-LSD -3 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 14435 14 3H-LSD -3 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
5090 15529 106 3H-LSD -1348 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15529 106 3H-LSD -1348 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5210 33308 48 3H-5HT -123 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 None
CHEMBL1200765 33308 48 3H-5HT -123 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 None
CHEMBL1419 33308 48 3H-5HT -123 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 5 0 1 4.7 CC(C)CC(N(C)C)C1(c2ccc(Cl)cc2)CCC1 None
156391 46770 99 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46770 99 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46770 99 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
4771 50500 29 3H-5HT 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 1 2.0 CC(C)(N)Cc1ccccc1 None
CHEMBL1574 50500 29 3H-5HT 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 1 2.0 CC(C)(N)Cc1ccccc1 None
2244 94204 100 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 94204 100 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
104870 98852 47 3H-MESULERGINE -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98852 47 3H-MESULERGINE -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98852 47 3H-MESULERGINE -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
43815 186896 64 3H-5HT -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186896 64 3H-5HT -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186896 64 3H-5HT -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
3672 192509 136 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 192509 136 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 193591 112 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 193591 112 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 196512 92 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 196512 92 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 200528 115 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 200528 115 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 200528 115 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
5281600 203002 92 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203002 92 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 203043 87 3H-5HT -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203043 87 3H-5HT -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
3821 204695 17 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 204695 17 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
4158 205318 21 3H-5HT -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205318 21 3H-5HT -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205318 21 3H-5HT -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 205478 72 3H-LSD -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205478 72 3H-LSD -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205478 72 3H-LSD -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
6852400 215914 0 3H-KETANSERIN -25118 22 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 215914 0 3H-KETANSERIN -25118 22 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
None 216316 0 3H-MESULERGINE -1862 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
135269 216363 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 216364 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 216365 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 216366 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 216367 0 3H-LSD -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 216368 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 216369 0 3H-LSD -7 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 216424 0 3H-5HT -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 4 1 1 4.6 CC(C)CC(C1(CCC1)C2=CC=C(C=C2)Cl)N.Cl None
None 216462 0 3H-LSD -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
1150 3849 121 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 3H-5HT -2 25 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
185 3975 60 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3975 60 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3975 60 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3975 60 3H-5HT -2344 38 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
62787 206165 21 3H-5HT -10 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 206165 21 3H-5HT -10 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
None 216109 0 3H-LSD -1122 24 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
102 4096 48 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -100 50 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
141 1415 35 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1415 35 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1415 35 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1415 35 3H-LSD -1 22 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
3668 216096 0 3H-LSD -977 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 510 5 4 9 0.4 CNC(=O)C1C(C(C(O1)N2C=NC3=C2N=CN=C3NCC4=CC(=CC=C4)I)O)O None
146 135 85 3H-5HT -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
164682 135 85 3H-5HT -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
CHEMBL275628 135 85 3H-5HT -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
1621 2413 17 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2413 17 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2413 17 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2413 17 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2413 17 3H-KETANSERIN -35 45 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
15897 2840 0 3H-LSD 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-LSD 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-LSD 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2840 0 3H-5-HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2840 0 3H-5HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-5-HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-5HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-5-HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-5HT 12 37 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
5 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -29 55 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
152 363 29 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 363 29 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 363 29 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
135398745 2893 112 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-5HT -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
152 363 29 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 363 29 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 363 29 3H-5HT 1 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
45486902 196923 0 UNDEFINED -3 2 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
CHEMBL566396 196923 0 UNDEFINED -3 2 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 449 5 2 4 4.6 O=c1[nH]c2cccc(OCC3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
1150 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
1150 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 3H-5HT -8 25 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
77590 215930 0 3H-5HT -15 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 124 4 0 2 0.8 COCCOCCl None
2389 3306 118 35S-GTPGammaS -66 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 35S-GTPGammaS -66 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 35S-GTPGammaS -66 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 35S-GTPGammaS -66 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 35S-GTPGammaS -66 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
542051 206077 6 3H-5HT -128 7 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8569 206077 6 3H-5HT -128 7 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
1809 134 32 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
5 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
199 391 0 3H-5HT -5 5 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
9821951 391 0 3H-5HT -5 5 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
CHEMBL160293 391 0 3H-5HT -5 5 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 None
135398745 2893 112 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 35S-GTPGammaS -5 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135 2515 43 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -3 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
7153 97992 77 3H-MESULERGINE -1 34 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-MESULERGINE -1 34 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
134 2497 24 125I-DOI -10 68 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 125I-DOI -10 68 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 125I-DOI -10 68 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 125I-DOI -10 68 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 125I-DOI -10 68 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
None 216423 0 Functional -1 28 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 216423 0 UNDEFINED -1 28 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 215922 0 3H-KETANSERIN -851 24 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
2202 3110 96 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3110 96 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3110 96 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3110 96 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3110 96 3H-MESULERGINE -6 21 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
221 3465 71 3H-5HT -4 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3465 71 3H-5HT -4 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3465 71 3H-5HT -4 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
5 139 72 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-DOI -2951 55 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1809 134 32 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -999 37 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
173 3238 95 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
None 216188 0 3H-5HT -120 15 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 438 5 1 4 4.8 C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45 None
179 399 115 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 399 115 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 399 115 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 399 115 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 399 115 3H-LSD -17 51 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
77379 19014 75 3H-5HT -2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
CHEMBL1288716 19014 75 3H-5HT -2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
102 4096 48 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-RAUWOLSCINE -93 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
5 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
77158 19015 56 3H-5HT 2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
CHEMBL1288717 19015 56 3H-5HT 2 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
None 217442 0 UNDEFINED -14 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 421 4 3 4 3.3 C1CC2=C(CC1CNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)C6=C(N2)C=CC(=C6)F None
145 140 49 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 3H-KETANSERIN -251 30 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1150 3849 121 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 3H-KETANSERIN -56 25 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
173 3238 95 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 3H-5HT -3 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
25058166 215935 0 3H-MESULERGINE -66 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215935 0 3H-MESULERGINE -66 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2470 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -14125 60 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 215922 0 3H-5HT -33 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
130 3474 47 3H-5HT -478 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3474 47 3H-5HT -478 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3474 47 3H-5HT -478 13 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
240 941 43 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 941 43 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 941 43 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 941 43 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 941 43 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 941 43 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 941 43 3H-5HT -26 25 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2105 3032 37 3H-LSD -28 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3032 37 3H-LSD -28 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3032 37 3H-LSD -28 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3032 37 3H-LSD -28 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3032 37 3H-LSD -28 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
138107169 215927 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
186 1794 52 3H-LSD -426 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1794 52 3H-LSD -426 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1794 52 3H-LSD -426 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
1353 1898 93 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 3H-5HT -295 86 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 215915 0 3H-5HT -2398 21 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1809 134 32 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
124 2960 47 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2960 47 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2960 47 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2960 47 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2960 47 3H-5HT -181 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
15897 2840 0 3H-LSD 12 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-LSD 12 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-LSD 12 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
138107169 215927 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-5HT -33 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 215915 0 3H-LSD -407 21 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1809 134 32 Functional -999 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 Functional -999 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 Functional -999 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
221 3465 71 UNDEFINED 4 14 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3465 71 UNDEFINED 4 14 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3465 71 UNDEFINED 4 14 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
6446436 216426 0 3H-MESULERGINE -1 2 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 3 4 3.2 CC1=CC2=C(C=C1)C(C3=C2N(C=C3)CC(C)N)(C)C.C(=CC(=O)O)C(=O)O None
134 2497 24 Functional -2 68 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 Functional -2 68 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 Functional -2 68 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 Functional -2 68 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 Functional -2 68 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1614 203632 24 Functional 2 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 203632 24 Functional 2 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
1809 134 32 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -1659 37 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107992 2536 49 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2536 49 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2536 49 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2536 49 3H-MESULERGINE -1 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
28 3470 46 3H-5HT -954 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 3470 46 3H-5HT -954 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 3470 46 3H-5HT -954 10 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
2470 3626 50 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -14125 60 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2389 3306 118 3H-LSD -66 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 3H-LSD -66 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 3H-LSD -66 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 3H-LSD -66 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 3H-LSD -66 68 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 121 3H-5HT -4 31 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -4 31 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -4 31 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
None 215922 0 3H-5HT -12 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 217444 0 UNDEFINED -12 3 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 432 3 2 4 3.8 C1CC2=C(CC1CN3CC4CC3CN4C5=CC=CC6=C5OC(=O)N6)C7=C(N2)C=CC(=C7)F None
105432 215999 0 3H-5HT -30 4 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 240 5 1 5 1.5 CC(CC1=CC(=C(C=C1OC)[N+](=O)[O-])OC)N None
18971832 2402 0 3H-5HT -263 13 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 2402 0 3H-5HT -263 13 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 2402 0 3H-5HT -263 13 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
37459 743 13 3H-KETANSERIN -39 25 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 743 13 3H-KETANSERIN -39 25 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 743 13 3H-KETANSERIN -39 25 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
None 215922 0 3H-5HT -12 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5268 3629 40 3H-RAUWOLSCINE -1047 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3629 40 3H-RAUWOLSCINE -1047 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3629 40 3H-RAUWOLSCINE -1047 18 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
173 3238 95 Functional 1 23 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 Functional 1 23 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 Functional 1 23 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1353 1898 93 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 3H-5HT -295 86 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
119607 206180 113 3H-LSD 97 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 206180 113 3H-LSD 97 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
1809 134 32 3H-5HT -999 37 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -999 37 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -999 37 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
31016 102260 15 3H-5HT -11 5 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
CHEMBL30336 102260 15 3H-5HT -11 5 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
213 3824 55 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3824 55 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3824 55 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3824 55 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3824 55 3H-LSD -5 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5 139 72 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
134 2497 24 3H-LSD -2 68 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-LSD -2 68 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-LSD -2 68 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-LSD -2 68 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-LSD -2 68 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
11957541 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
7153 97992 77 3H-LSD -1 34 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-LSD -1 34 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
135 2515 43 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -3 58 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
3652 4066 79 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4066 79 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4066 79 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4066 79 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4066 79 3H-5HT -2 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
5268 3629 40 3H-5HT -616 18 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3629 40 3H-5HT -616 18 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3629 40 3H-5HT -616 18 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
1574 81 60 3H-5HT -2 21 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 3H-5HT -2 21 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 3H-5HT -2 21 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
135 2515 43 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -37 58 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1150 3849 121 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
1150 3849 121 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 125I-DOI -8 25 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 3H-5HT -8 25 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
152 363 29 Functional 1 19 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 363 29 Functional 1 19 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 363 29 Functional 1 19 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
5 139 72 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 Functional -13 55 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4106 2485 22 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2485 22 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2485 22 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2485 22 3H-5HT -3 34 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5074 3307 80 3H-5HT -2 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -2 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -2 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -2 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
None 216026 0 3H-LSD -2 8 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 339 4 3 3 1.9 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
133 2479 52 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2479 52 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2479 52 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2479 52 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2479 52 3H-KETANSERIN -4 43 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1524 2168 96 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-KETANSERIN -1 52 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
None 216354 0 3H-5HT 5 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
191 3472 52 3H-5HT -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 None
443389 3472 52 3H-5HT -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 None
CHEMBL276140 3472 52 3H-5HT -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 None
None 216353 0 3H-5HT -2 11 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
135409468 2022 69 3H-LSD 1 40 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2022 69 3H-LSD 1 40 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2022 69 3H-LSD 1 40 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
5 139 72 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-MESULERGINE -13 55 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
155 725 25 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 725 25 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 725 25 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 725 25 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 725 25 Functional -5 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
1588 2311 27 3H-LSD -6 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2311 27 3H-LSD -6 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2311 27 3H-LSD -6 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2311 27 3H-LSD -6 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2311 27 3H-LSD -6 44 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
None 216252 0 3H-LSD -32 12 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
11957541 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
11957541 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-5HT -2 16 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1615 167767 24 Functional -2 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167767 24 Functional -2 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
2389 3306 118 3H-5HT -549 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 3H-5HT -549 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 3H-5HT -549 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 3H-5HT -549 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 3H-5HT -549 68 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1524 2168 96 125I-DOI -154 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 125I-DOI -154 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 125I-DOI -154 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 125I-DOI -154 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 125I-DOI -154 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 125I-DOI -154 52 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
189 3466 39 3H-LSD -5 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3466 39 3H-LSD -5 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3466 39 3H-LSD -5 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
155 725 25 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 725 25 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 725 25 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 725 25 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 725 25 3H-5HT -10 13 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
202 1496 77 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1496 77 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1496 77 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1496 77 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1496 77 3H-5HT -1 33 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
2477 742 59 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 742 59 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 742 59 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 742 59 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 742 59 3H-5HT -13 29 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
1524 2168 96 3H-RAUWOLSCINE -229 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-RAUWOLSCINE -229 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-RAUWOLSCINE -229 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-RAUWOLSCINE -229 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-RAUWOLSCINE -229 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-RAUWOLSCINE -229 52 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2176 3104 68 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3104 68 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3104 68 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3104 68 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3104 68 3H-5HT -933 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
277 1289 62 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1289 62 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1289 62 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1289 62 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1289 62 125I-DOI -26 46 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
189 3466 39 3H-5HT -5 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3466 39 3H-5HT -5 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3466 39 3H-5HT -5 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
1220 187 55 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-5HT -1905 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
6917970 3665 61 3H-LSD -51 34 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3665 61 3H-LSD -51 34 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3665 61 3H-LSD -51 34 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
1524 2168 96 3H-MESULERGINE -229 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-MESULERGINE -229 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-MESULERGINE -229 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-MESULERGINE -229 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-MESULERGINE -229 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-MESULERGINE -229 52 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
104911 215994 0 3H-LSD -99 38 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
105432 215999 0 3H-5HT -44 4 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 240 5 1 5 1.5 CC(CC1=CC(=C(C=C1OC)[N+](=O)[O-])OC)N None
1150 3849 121 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 3H-5HT -2 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
7153 97992 77 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
7153 97992 77 UNDEFINED -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 UNDEFINED -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 216423 0 UNDEFINED -1 28 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
198 312 126 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 312 126 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 312 126 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 312 126 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 312 126 3H-MESULERGINE -346 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
None 215922 0 Functional -33 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
11957541 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
7153 97992 77 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
6166 215998 0 3H-5HT -7 4 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 330 2 1 3 3.7 C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)CO)CCC4=CC(=O)CC[C@]34C None
155 725 25 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 725 25 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 725 25 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 725 25 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 725 25 3H-5HT -5 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
7153 97992 77 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
57174031 215917 0 3H-KETANSERIN -457 20 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
185 3975 60 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3975 60 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3975 60 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3975 60 3H-LSD -2344 38 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
3294 1993 111 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1993 111 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1993 111 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1993 111 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1993 111 3H-LSD -38 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
3337 206344 27 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-LSD -75 41 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
2865 4112 73 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4112 73 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4112 73 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4112 73 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4112 73 3H-5HT -12 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
11957541 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-5HT -6 16 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
5 139 72 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -29 55 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
11957541 1446 40 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-5HT -2 16 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
7153 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
7153 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
138107169 215927 0 3H-5HT -33 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-5HT -33 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
1574 81 60 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1574 81 60 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 3H-5HT -3 21 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
115 3762 80 Functional -1 27 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3762 80 Functional -1 27 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3762 80 Functional -1 27 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2389 3306 118 3H-5HT -66 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 3H-5HT -66 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 3H-5HT -66 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 3H-5HT -66 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 3H-5HT -66 68 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1150 3849 121 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 Functional -2 25 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
107992 2536 49 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2536 49 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2536 49 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2536 49 Functional -1 10 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
11954224 215928 0 3H-5HT -66 60 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 216423 0 3H-MESULERGINE 1 28 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
7153 97992 77 3H-5HT -1 34 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1342 36 49 3H-5HT 2 19 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 49 3H-5HT 2 19 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 49 3H-5HT 2 19 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
206 2476 16 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
135398737 955 93 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-RAUWOLSCINE -2 92 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
206 2476 16 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-5HT -1 25 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
242 469 124 3H-LSD -1 52 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 3H-LSD -1 52 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 3H-LSD -1 52 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 3H-LSD -1 52 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 3H-LSD -1 52 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
11954224 215928 0 3H-5HT -66 60 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
206 2476 16 3H-5HT -1 25 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-5HT -1 25 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-5HT -1 25 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
5074 3307 80 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 125I-DOI -6 30 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1342 36 49 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 49 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 49 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1621 2413 17 3H-LSD -19 45 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2413 17 3H-LSD -19 45 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2413 17 3H-LSD -19 45 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2413 17 3H-LSD -19 45 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2413 17 3H-LSD -19 45 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1342 36 49 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 49 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 49 3H-5HT 2 19 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1621 2413 17 3H-LSD -39 45 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2413 17 3H-LSD -39 45 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2413 17 3H-LSD -39 45 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2413 17 3H-LSD -39 45 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2413 17 3H-LSD -39 45 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
None 215915 0 Functional -407 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
6971132 215984 0 3H-LSD -7 14 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
219050 3348 25 3H-MESULERGINE -194 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3348 25 3H-MESULERGINE -194 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3348 25 3H-MESULERGINE -194 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
2470 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2 3237 23 3H-5HT -363 29 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3237 23 3H-5HT -363 29 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3237 23 3H-5HT -363 29 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
186 1794 52 3H-5HT -426 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1794 52 3H-5HT -426 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1794 52 3H-5HT -426 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
31016 102260 15 3H-5HT -5 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
CHEMBL30336 102260 15 3H-5HT -5 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 225 5 1 4 1.6 COc1cc(CC(C)N)cc(OC)c1OC None
135398737 955 93 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-5HT -36 92 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
102 4096 48 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -93 50 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
7153 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 215922 0 3H-5HT -33 24 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
6166 215998 0 3H-5HT -4 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 330 2 1 3 3.7 C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)CO)CCC4=CC(=O)CC[C@]34C None
1574 81 60 3H-5HT -3 21 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 3H-5HT -3 21 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 3H-5HT -3 21 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
130 3474 47 35S-GTPGammaS -478 13 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3474 47 35S-GTPGammaS -478 13 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3474 47 35S-GTPGammaS -478 13 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
2470 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1524 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2470 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3626 50 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-RAUWOLSCINE -14125 60 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
7153 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1524 2168 96 3H-5HT -229 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -229 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -229 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -229 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -229 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -229 52 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2470 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
15760 113052 57 3H-5HT -5 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 174 2 2 1 2.0 Cc1ccc2[nH]cc(CCN)c2c1 None
CHEMBL331241 113052 57 3H-5HT -5 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 174 2 2 1 2.0 Cc1ccc2[nH]cc(CCN)c2c1 None
None 215915 0 3H-LSD -407 21 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
186 1794 52 3H-5HT -426 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1794 52 3H-5HT -426 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1794 52 3H-5HT -426 17 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
2470 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -120226 60 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
138107169 215927 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
138107169 215927 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-5HT -117 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
206 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
1524 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -2691 52 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
206 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
7153 97992 77 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1353 1898 93 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 3H-5HT -295 86 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1524 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2168 96 3H-KETANSERIN -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-KETANSERIN -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-KETANSERIN -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-KETANSERIN -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-KETANSERIN -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-KETANSERIN -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2220 3112 82 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 3112 82 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 3112 82 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 3112 82 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 3112 82 3H-5HT -10 14 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
77158 19015 56 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
CHEMBL1288717 19015 56 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
2402 3345 62 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3345 62 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3345 62 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3345 62 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3345 62 3H-MESULERGINE -9 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
145 140 49 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 3H-LSD -87 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
77158 19015 56 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
CHEMBL1288717 19015 56 3H-5HT -2 2 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 None
206 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-5HT -26 25 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
138107169 215927 0 3H-5HT -117 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-5HT -117 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
115 3762 80 3H-5HT -1 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3762 80 3H-5HT -1 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3762 80 3H-5HT -1 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
3337 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
1524 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -229 52 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
102 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -93 50 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
1524 2168 96 3H-5HT -2691 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -2691 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -2691 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -2691 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -2691 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -2691 52 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5 139 72 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135398737 955 93 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-LSD -2 92 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
138107169 215927 0 3H-RAUWOLSCINE -33 23 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-RAUWOLSCINE -33 23 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
135 2515 43 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -3 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2865 4112 73 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4112 73 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4112 73 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4112 73 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4112 73 3H-LSD -12 54 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1342 36 49 3H-5HT -4 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 49 3H-5HT -4 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 49 3H-5HT -4 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3117 207818 103 None -8 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 207818 103 None -8 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
104903 56314 17 None -4 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
CHEMBL1630578 56314 17 None -4 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
7153 97992 77 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
102 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
7153 97992 77 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-5HT -1 34 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
164 1448 19 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
85875 1448 19 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
CHEMBL8600 1448 19 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
DB01528 1448 19 3H-KETANSERIN -17 10 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
3337 206344 27 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 Functional -75 41 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
None 217441 0 UNDEFINED -83 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 449 6 3 4 4.1 C1CC2=C(CC1CCCNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)NC6=C2C=C(C=C6)F None
107992 2536 49 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2536 49 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2536 49 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2536 49 3H-5HT -5 10 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
1220 187 55 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-5HT -1905 45 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
11848624 89117 0 UNDEFINED 2 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL236587 89117 0 UNDEFINED 2 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
2389 3306 118 3H-LSD -66 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 3H-LSD -66 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 3H-LSD -66 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 3H-LSD -66 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 3H-LSD -66 68 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1220 187 55 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-5HT -3235 45 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3337 206344 27 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-5HT -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-LSD -75 41 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
1210 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 915 51 3H-RAUWOLSCINE -1380 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
102 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
155 725 25 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 725 25 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 725 25 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 725 25 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 725 25 3H-5HT -5 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
102 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -93 50 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
11954224 215928 0 3H-LSD -66 60 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11291 3196 26 3H-KETANSERIN -44 5 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C None
4980 3196 26 3H-KETANSERIN -44 5 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C None
CHEMBL65547 3196 26 3H-KETANSERIN -44 5 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C None
None 216423 0 3H-5HT 1 28 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
173 3238 95 3H-KETANSERIN -5 23 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 3H-KETANSERIN -5 23 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 3H-KETANSERIN -5 23 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
2181 3106 46 3H-5HT -15 35 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3106 46 3H-5HT -15 35 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3106 46 3H-5HT -15 35 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3106 46 3H-5HT -15 35 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3106 46 3H-5HT -15 35 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
15897 2840 0 3H-5-HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2840 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-5-HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-5-HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
186 1794 52 3H-5HT -776 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1794 52 3H-5HT -776 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1794 52 3H-5HT -776 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
5268 3629 40 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3629 40 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3629 40 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
15897 2840 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
173 3238 95 3H-5HT 1 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 3H-5HT 1 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 3H-5HT 1 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
11653679 181167 1 UNDEFINED -75 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 181167 1 UNDEFINED -75 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
10836 14435 14 None -3 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 14435 14 None -3 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
5475158 67183 25 3H-KETANSERIN -1 14 Bovine 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 67183 25 3H-KETANSERIN -1 14 Bovine 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
5074 3307 80 3H-5HT -2 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5074 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -2 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -2 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -2 30 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5870 31630 92 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O None
CHEMBL1405 31630 92 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 270 0 1 2 3.8 C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O None
None 216354 0 3H-5HT 5 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
5074 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2812 4747 101 None -40 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4747 101 None -40 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
222757 99348 73 None -1 3 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O None
CHEMBL282575 99348 73 None -1 3 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O None
1210 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 915 51 None -1380 21 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
5074 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -8 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1357 2468 139 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2468 139 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2468 139 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2468 139 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2468 139 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2468 139 None -3890 9 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1342 36 49 3H-5HT -4 19 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 49 3H-5HT -4 19 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 49 3H-5HT -4 19 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1209 1645 75 None -199 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1645 75 None -199 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1645 75 None -199 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1645 75 None -199 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1645 75 None -199 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3198 205490 76 None -30 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 205490 76 None -30 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 205490 76 None -30 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2406 100376 89 None -27 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
CHEMBL290106 100376 89 None -27 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O None
None 216354 0 3H-5HT 5 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 342 4 3 4 2.5 CC(CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=CC(=O)O)C(=O)O None
66265 93984 15 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 93984 15 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
1836 2574 59 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 2574 59 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 2574 59 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 2574 59 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 2574 59 None -69 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
2402 3345 62 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3345 62 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3345 62 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3345 62 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3345 62 None -9 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
3598 187797 76 None -2 7 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl None
CHEMBL496 187797 76 None -2 7 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl None
135 2515 43 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-RAUWOLSCINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4189 206899 96 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 206899 96 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 206899 96 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
4943 193393 105 None 1 2 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O None
CHEMBL526 193393 105 None 1 2 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 178 2 1 1 3.6 CC(C)c1cccc(C(C)C)c1O None
3336 94972 30 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL1405922 94972 30 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL254832 94972 30 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
135 2515 43 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-MESULERGINE -3 58 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
189 3466 39 3H-MESULERGINE -5 17 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3466 39 3H-MESULERGINE -5 17 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3466 39 3H-MESULERGINE -5 17 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
4211 57792 83 None -2 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
CHEMBL1670 57792 83 None -2 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
5353853 17954 47 None -23 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 17954 47 None -23 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 17954 47 None -23 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1599 2326 50 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2326 50 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2326 50 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2326 50 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2326 50 None -144 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
4209 3141 75 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3141 75 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3141 75 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3141 75 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3141 75 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3141 75 None -758 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
2142 3074 58 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3074 58 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3074 58 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3074 58 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3074 58 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3074 58 None -43 37 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
146 135 85 3H-5HT 1 3 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
164682 135 85 3H-5HT 1 3 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
CHEMBL275628 135 85 3H-5HT 1 3 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 None
68617 205504 62 None -15 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205504 62 None -15 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205504 62 None -15 26 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
4601 206724 35 None -4 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206724 35 None -4 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206724 35 None -4 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
448537 160226 89 None -21 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 160226 89 None -21 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
2176 3104 68 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3104 68 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3104 68 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3104 68 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3104 68 None -933 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1531 2253 69 None -16 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2253 69 None -16 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2253 69 None -16 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2253 69 None -16 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2253 69 None -16 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
5318 15544 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1200348 15544 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1221 15544 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
119607 206180 113 None 97 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 206180 113 None 97 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
1227 2472 43 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2472 43 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2472 43 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2472 43 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2472 43 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2472 43 None -112 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3151 1450 97 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1450 97 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1450 97 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1450 97 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1450 97 None -125 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
1343 1876 62 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
3519 1876 62 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
522 1876 62 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
CHEMBL862 1876 62 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
DB01018 1876 62 None -14 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N None
1016 3720 78 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3720 78 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3720 78 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3720 78 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3720 78 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3720 78 None -17 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5510 205829 100 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 None
CHEMBL83668 205829 100 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 2 0 2 4.9 Cc1cccc(N(C)C(=S)Oc2ccc3ccccc3c2)c1 None
2202 3110 96 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3110 96 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3110 96 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3110 96 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3110 96 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
2723 154022 108 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl None
CHEMBL398440 154022 108 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl None
2771 194994 74 None 1 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 194994 74 None 1 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 194994 74 None 1 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2333 142310 97 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 None
CHEMBL388590 142310 97 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 None
135 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2470 3626 50 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 125I-DOI -1513 60 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
102 4096 48 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -93 50 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
135 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
221 3465 71 UNDEFINED 4 14 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3465 71 UNDEFINED 4 14 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3465 71 UNDEFINED 4 14 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
102 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
1615 167767 24 3H-LSD -2 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167767 24 3H-LSD -2 45 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
122 1425 9 3H-5HT -100 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
156314 1425 9 3H-5HT -100 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL1332062 1425 9 3H-5HT -100 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
1209 1645 75 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1645 75 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1645 75 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1645 75 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1645 75 3H-5HT -199 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
5268 3629 40 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3629 40 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3629 40 3H-5HT -1047 18 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
208 2843 0 3H-5HT -69 13 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2843 0 3H-5HT -69 13 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2843 0 3H-5HT -69 13 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3337 206344 27 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-5-HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
221 3465 71 3H-MESULERGINE -4 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3465 71 3H-MESULERGINE -4 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3465 71 3H-MESULERGINE -4 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3337 206344 27 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-LSD -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
108182 4100 22 3H-5HT -1 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 4100 22 3H-5HT -1 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 4100 22 3H-5HT -1 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
15897 2840 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-LSD 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
15897 2840 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-5HT 12 37 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
135 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
135 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -37 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 216000 0 3H-5HT -5 4 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2105 3032 37 Functional -28 33 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3032 37 Functional -28 33 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3032 37 Functional -28 33 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3032 37 Functional -28 33 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3032 37 Functional -28 33 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
102 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
135398745 2893 112 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-5HT -27 66 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11957541 1446 40 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-5HT -2 16 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
102 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 3H-5HT -100 50 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
542051 206077 6 3H-5HT -61 7 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8569 206077 6 3H-5HT -61 7 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
1220 187 55 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-KETANSERIN -4265 45 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3337 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-5HT -75 41 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
11957541 1446 40 3H-KETANSERIN -16 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-KETANSERIN -16 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-KETANSERIN -16 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-KETANSERIN -16 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-KETANSERIN -16 16 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
141 1415 35 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1415 35 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1415 35 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1415 35 3H-KETANSERIN -6 22 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
31101 726 40 3H-MESULERGINE -26 36 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 726 40 3H-MESULERGINE -26 36 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 726 40 3H-MESULERGINE -26 36 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 726 40 3H-MESULERGINE -26 36 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 726 40 3H-MESULERGINE -26 36 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
2181 3106 46 3H-5HT -478 35 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3106 46 3H-5HT -478 35 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3106 46 3H-5HT -478 35 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3106 46 3H-5HT -478 35 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3106 46 3H-5HT -478 35 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
3337 206344 27 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337 206344 27 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337 206344 27 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-5-HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-5HT -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-LSD -75 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
1357 2468 139 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2468 139 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2468 139 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2468 139 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2468 139 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2468 139 3H-MESULERGINE -3890 9 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
115 3762 80 3H-5HT -1 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3762 80 3H-5HT -1 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3762 80 3H-5HT -1 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
138107169 215927 0 3H-5HT -117 23 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215927 0 3H-5HT -117 23 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
2470 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
283 3108 57 3H-5HT -562 12 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 3108 57 3H-5HT -562 12 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 3108 57 3H-5HT -562 12 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
2726 916 68 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 916 68 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 916 68 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 916 68 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 916 68 3H-KETANSERIN -3 73 Bovine 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
None 217442 0 UNDEFINED -14 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 421 4 3 4 3.3 C1CC2=C(CC1CNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)C6=C(N2)C=CC(=C6)F None
44112 121264 48 None -11 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 None
CHEMBL357995 121264 48 None -11 7 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 None
1548955 88552 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88552 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88552 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
3168 9230 92 None -107 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9230 92 None -107 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
3042 1402 35 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1402 35 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1402 35 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1402 35 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1402 35 None -39 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
5591 157507 90 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 None
CHEMBL408 157507 90 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 None
1353 1898 93 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 None -295 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
4452 2742 19 3H-LSD -208 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2742 19 3H-LSD -208 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2742 19 3H-LSD -208 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
4178 195780 63 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N None
CHEMBL558 195780 63 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 179 3 1 2 2.0 Cc1cccc(C)c1OCC(C)N None
1224 1420 83 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1420 83 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1420 83 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1420 83 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1420 83 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1420 83 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
146159245 188426 30 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
451415 188426 30 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
86289437 188426 30 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
CHEMBL502620 188426 30 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 811 9 4 16 3.2 CC[C@@]1(O)C[C@H](O[C@H]2C[C@H](N(C)C)[C@H](O[C@H]3C[C@H](O)[C@H](O[C@H]4CCC(=O)[C@H](C)O4)[C@H](C)O3)[C@H](C)O2)c2c(cc3c(c2O)C(=O)c2c(O)cccc2C3=O)[C@H]1C(=O)OC None
12488 1644 56 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 1644 56 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 1644 56 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 1644 56 None -11 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
3033538 1307 39 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
7155 1307 39 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
781 1307 39 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
CHEMBL1201216 1307 39 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
DB00298 1307 39 None -12 9 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 None
77379 19014 75 3H-5HT 2 2 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
CHEMBL1288716 19014 75 3H-5HT 2 2 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 None
657255 199061 34 None -9 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 199061 34 None -9 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
176 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
4098 32475 30 None -14 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1255739 32475 30 None -14 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1411979 32475 30 None -14 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
5282379 194961 69 None 1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 None
CHEMBL547 194961 69 None 1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1 None
134 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2028 2958 80 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2958 80 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2958 80 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2958 80 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2958 80 None -40 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
134 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -12 68 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
6437377 215929 0 3H-5HT -5 5 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
1547484 937 74 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 937 74 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 937 74 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 937 74 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 937 74 None -8 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
4595 176691 106 None 2 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 176691 106 None 2 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
1782 2501 84 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 2501 84 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 2501 84 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 2501 84 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 2501 84 None -3 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
2477 742 59 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 742 59 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 742 59 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 742 59 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 742 59 None -13 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
5074 3307 80 3H-5HT -2 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3307 80 3H-5HT -2 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3307 80 3H-5HT -2 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3307 80 3H-5HT -2 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
6075 150084 42 None -8 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 150084 42 None -8 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
2470 3626 50 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 None -14125 60 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
198 312 126 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 312 126 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 312 126 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 312 126 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 312 126 None -346 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
210 3451 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
2423 3451 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
5160 3451 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
CHEMBL52939 3451 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
DB12163 3451 0 None -7 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C None
133 2479 52 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2479 52 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2479 52 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2479 52 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2479 52 3H-5HT -12 43 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
6726 1269 51 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 1269 51 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 1269 51 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 1269 51 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 1269 51 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
3157 1458 71 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
7170 1458 71 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
954 1458 71 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
CHEMBL707 1458 71 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
DB00590 1458 71 None -37 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
444795 139974 105 None 3 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 None
CHEMBL38 139974 105 None 3 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 None
2284 3160 33 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3160 33 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3160 33 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3160 33 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3160 33 None -16 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
165193 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3165 68 None -72 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4011 82379 49 None -20 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82379 49 None -20 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
3191 102831 97 None -7 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102831 97 None -7 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
1524 2168 96 None -229 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 None -229 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 None -229 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 None -229 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 None -229 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 None -229 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
119584 2577 102 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
1848 2577 102 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
242 2577 102 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
CHEMBL60889 2577 102 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
DB11675 2577 102 None 1 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 421 7 2 5 3.1 CCOc1cc(N)c(cc1C(=O)NCC1OCCN(C1)Cc1ccc(cc1)F)Cl None
33630 178933 99 None -6 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178933 99 None -6 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
1605 2327 117 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
3957 2327 117 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
7216 2327 117 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
CHEMBL998 2327 117 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
DB00455 2327 117 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
2895 203569 41 None 1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
CHEMBL669 203569 41 None 1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
2398 951 62 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 951 62 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 951 62 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 951 62 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 951 62 None -3 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
1222 1651 49 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1651 49 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1651 49 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1651 49 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1651 49 None -52 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
11658860 2329 51 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
2941 2329 51 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
4374 2329 51 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
CHEMBL360328 2329 51 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
DB04871 2329 51 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 None
124 2960 47 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2960 47 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2960 47 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2960 47 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2960 47 None -181 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
6437377 215929 0 3H-5HT -5 5 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
1201549 594 24 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 594 24 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 594 24 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 594 24 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 594 24 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 594 24 None -26 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
228 444 28 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 444 28 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 444 28 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 444 28 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 444 28 None -5 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
152 363 29 3H-5HT 1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 363 29 3H-5HT 1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 363 29 3H-5HT 1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2520 203985 70 None -4 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL1280 203985 70 None -4 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL6966 203985 70 None -4 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
15897 2840 0 Functional 12 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 Functional 12 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 Functional 12 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
None 215916 0 3H-KETANSERIN -19 6 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 6 2 7 2.1 CC(C1=CC=CC2=NC3=C(C=CC=C3N=C21)C(=O)O)OC(=O)C(CO)OC None
10624 70271 19 3H-KETANSERIN -46 33 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 70271 19 3H-KETANSERIN -46 33 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 70271 19 3H-KETANSERIN -46 33 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
71285 215960 0 Functional 1 2 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 209 3 2 4 1.3 CC(CC1=CC2=C(C=C1O)OCO2)NC None
283 3108 57 3H-5HT -57 12 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 3108 57 3H-5HT -57 12 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 3108 57 3H-5HT -57 12 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
115237 55555 119 3H-LSD -89 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55555 119 3H-LSD -89 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
None 217441 0 UNDEFINED -83 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 449 6 3 4 4.1 C1CC2=C(CC1CCCNCC3COC4=C(O3)C=CC5=C4CC(=O)N5)NC6=C2C=C(C=C6)F None
107992 2536 49 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2536 49 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2536 49 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2536 49 3H-5HT -1 10 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
240 941 43 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 941 43 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 941 43 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 941 43 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 941 43 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 941 43 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 941 43 3H-5HT -6 25 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
7153 97992 77 Functional -1 34 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 Functional -1 34 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 216423 0 Functional 1 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
107780 1831 54 3H-5HT -676 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1831 54 3H-5HT -676 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1831 54 3H-5HT -676 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1524 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -229 52 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
173 3238 95 3H-5HT -3 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 3H-5HT -3 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 3H-5HT -3 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1574 81 60 125I-DOI -70 21 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 125I-DOI -70 21 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 125I-DOI -70 21 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
173 3238 95 125I-DOI -75 23 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 125I-DOI -75 23 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 125I-DOI -75 23 Mouse 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1342 36 49 3H-5HT -4 19 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 49 3H-5HT -4 19 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 49 3H-5HT -4 19 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
44626329 197385 0 UNDEFINED -20 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
CHEMBL569513 197385 0 UNDEFINED -20 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 420 3 2 4 3.7 O=c1[nH]c2cccc(N3CCN(CC4CCc5[nH]c6ccc(F)cc6c5C4)CC3)c2o1 None
3337 206344 27 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-LSD -75 41 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
1210 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 915 51 3H-5HT -1380 21 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
62787 206165 21 3H-KETANSERIN -67 10 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 206165 21 3H-KETANSERIN -67 10 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
2470 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5440 28693 37 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 None
CHEMBL1378 28693 37 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 None
4976 203556 29 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 203556 29 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
5022 1638 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
6918248 1638 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
8182 1638 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
CHEMBL231068 1638 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
DB04908 1638 76 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
1971 2846 38 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2846 38 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2846 38 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2846 38 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2846 38 None -4 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
107 141 121 3H-5HT -12 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -12 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -12 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
213 3824 55 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3824 55 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3824 55 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3824 55 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3824 55 None -5 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
11957541 1446 40 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1446 40 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1446 40 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1446 40 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1446 40 3H-MESULERGINE -2 16 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
2105 3032 37 3H-MESULERGINE -28 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3032 37 3H-MESULERGINE -28 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3032 37 3H-MESULERGINE -28 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3032 37 3H-MESULERGINE -28 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3032 37 3H-MESULERGINE -28 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2601 3751 33 3H-MESULERGINE -8 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3751 33 3H-MESULERGINE -8 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3751 33 3H-MESULERGINE -8 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3751 33 3H-MESULERGINE -8 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3751 33 3H-MESULERGINE -8 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
100 3776 58 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3776 58 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3776 58 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3776 58 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3776 58 None -11 56 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
240 941 43 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 941 43 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 941 43 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 941 43 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 941 43 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 941 43 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 941 43 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
135398737 955 93 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-5HT -2 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2351 3261 64 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3261 64 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3261 64 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3261 64 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3261 64 None -7 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2274 3151 58 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3151 58 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3151 58 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3151 58 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3151 58 None -10 32 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2099 9275 55 None - 1 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL1110 9275 55 None - 1 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 294 2 1 3 2.4 Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O None
135398745 2893 112 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-LSD -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3952 1875 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5353646 1875 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5443 1875 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
5702063 1875 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL1331786 1875 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
CHEMBL420 1875 38 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N None
115237 55555 119 None -89 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55555 119 None -89 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
2291 3162 58 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3162 58 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3162 58 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3162 58 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3162 58 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
216239 23763 118 None 2 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1200485 23763 118 None 2 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1336 23763 118 None 2 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT2B receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
2726 916 68 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 916 68 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 916 68 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 916 68 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 916 68 None -19 73 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
31101 726 40 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 726 40 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 726 40 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 726 40 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 726 40 None -26 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
102 4096 48 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 None -100 50 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2181 3106 46 None -15 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3106 46 None -15 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3106 46 None -15 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3106 46 None -15 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3106 46 None -15 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
2286 3161 51 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3161 51 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3161 51 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3161 51 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3161 51 None -5 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
180 400 56 None -35 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 400 56 None -35 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 400 56 None -35 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 400 56 None -35 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 400 56 None -35 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2389 3306 118 None -66 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 None -66 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 None -66 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 None -66 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 None -66 68 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
114948 60267 14 None -1 3 Human 8.1 pKi = 8.1 Binding
Biased for β-arrestin signalling.Biased for β-arrestin signalling.
Drug Central 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 None
CHEMBL1743263 60267 14 None -1 3 Human 8.1 pKi = 8.1 Binding
Biased for β-arrestin signalling.Biased for β-arrestin signalling.
Drug Central 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 None
6761 67770 19 None -7 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67770 19 None -7 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
1621 2413 17 None -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2413 17 None -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2413 17 None -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2413 17 None -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2413 17 None -19 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligandBinding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2600 3750 74 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3750 74 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3750 74 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3750 74 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3750 74 None -1 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
1530 2169 50 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2169 50 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2169 50 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2169 50 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2169 50 None -19 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
124087 1377 114 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1377 114 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1377 114 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1377 114 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1377 114 None -5 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
2865 4112 73 None -12 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4112 73 None -12 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4112 73 None -12 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4112 73 None -12 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4112 73 None -12 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
135398737 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 1649 50 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1649 50 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1649 50 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1649 50 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1649 50 None -27 66 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
26987 946 33 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 946 33 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 946 33 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 946 33 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 946 33 None -47 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2267 557 71 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
271 557 71 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
7121 557 71 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
CHEMBL639 557 71 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
DB00972 557 71 None -10 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsDisplacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
3652 4066 79 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4066 79 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4066 79 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4066 79 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4066 79 None -2 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
2585 800 103 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 800 103 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 800 103 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 800 103 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 800 103 None -18 22 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
102 4096 48 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4096 48 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4096 48 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4096 48 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4096 48 None -93 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
135398745 2893 112 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 None -5 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
134 2497 24 3H-5HT -2 68 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -2 68 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -2 68 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -2 68 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -2 68 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
3036864 202731 19 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 202731 19 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 202731 19 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 202731 19 Functional -295 28 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1615 167767 24 3H-LSD -2 45 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167767 24 3H-LSD -2 45 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
2470 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3626 50 3H-5HT -14125 60 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1210 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 915 51 3H-5HT -1380 21 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1150 3849 121 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3849 121 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3849 121 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3849 121 3H-5HT -2 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
213 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
21830793 91806 10 3H-8-OH-DPAT -489 46 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91806 10 3H-8-OH-DPAT -489 46 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
45266826 217664 0 [3H] LSD 2 8 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 177 3 1 2 1.8 CC1=CC=C(C=C1)C(=O)C(C)NC None
179 399 115 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 399 115 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 399 115 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 399 115 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 399 115 3H-LSD -17 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
24740863 89129 0 UNDEFINED 1 6 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
CHEMBL236610 89129 0 UNDEFINED 1 6 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
1524 2168 96 3H-5HT -229 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2168 96 3H-5HT -229 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2168 96 3H-5HT -229 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2168 96 3H-5HT -229 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2168 96 3H-5HT -229 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2168 96 3H-5HT -229 52 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5 139 72 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-KETANSERIN -1778 55 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
77590 215930 0 3H-5HT -10 6 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 124 4 0 2 0.8 COCCOCCl None
221 3465 71 3H-5HT -4 14 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3465 71 3H-5HT -4 14 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3465 71 3H-5HT -4 14 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
None 216423 0 UNDEFINED 1 28 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
206 2476 16 3H-KETANSERIN -5 25 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2476 16 3H-KETANSERIN -5 25 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2476 16 3H-KETANSERIN -5 25 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
134551 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 357 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
135 2515 43 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 None -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2247 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 504 81 None -4 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1385580 29245 76 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
4615 29245 76 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
CHEMBL13828 29245 76 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
191 402 98 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 402 98 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 402 98 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 402 98 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 402 98 None -5 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2601 3751 33 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3751 33 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3751 33 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3751 33 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3751 33 None -8 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
135398737 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 None -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10531 1408 21 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1408 21 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1408 21 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1408 21 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1408 21 None -15 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
107715 200922 22 None -14 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 200922 22 None -14 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 200922 22 None -14 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
135526515 217697 0 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 301 7 4 3 2.8 CCCCCNC(=N)NN=CC1=CNC2=C1C=C(OC)C=C2 None
1588 2311 27 None -6 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2311 27 None -6 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2311 27 None -6 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2311 27 None -6 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2311 27 None -6 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
135398737 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-5HT -2 92 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1042 1568 23 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 1568 23 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 1568 23 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 1568 23 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 1568 23 None -7 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
2220 3112 82 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 3112 82 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 3112 82 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 3112 82 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 3112 82 None -1 14 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysisDisplacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis
Drug Central 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
3337 206344 27 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 Functional -75 41 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
11978813 718 79 None -2 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 718 79 None -2 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 718 79 None -2 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 718 79 None -2 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 718 79 None -2 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
133 2479 52 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2479 52 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2479 52 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2479 52 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2479 52 None -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
277 1289 62 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1289 62 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1289 62 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1289 62 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1289 62 None -5 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
37 775 60 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 775 60 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 775 60 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 775 60 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 775 60 None 1 17 Human 8.1 pKi = 8.1 Binding
Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysisDisplacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
11954224 215928 0 None -66 60 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1621 2413 17 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2413 17 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2413 17 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2413 17 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2413 17 Functional -19 45 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
135 2515 43 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -3 58 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 215944 0 3H-KETANSERIN -147 2 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 5 1 3 2.6 CCC1=CC(=C(C=C1OC)CC(C)N)OC.Cl None
3036864 202731 19 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 202731 19 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 202731 19 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 202731 19 3H-5HT -346 28 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
213 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3824 55 3H-5HT -5 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
115 3762 80 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3762 80 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3762 80 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
173 3238 95 3H-5HT 1 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3238 95 3H-5HT 1 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3238 95 3H-5HT 1 23 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
115 3762 80 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3762 80 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3762 80 3H-5HT -2 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2337 3232 77 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-LSD -15 63 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
134 2497 24 3H-5HT -12 68 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -12 68 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -12 68 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -12 68 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -12 68 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
119376 1828 48 3H-5HT -4786 27 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 1828 48 3H-5HT -4786 27 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 1828 48 3H-5HT -4786 27 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
71299720 215926 0 3H-5HT -691 17 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
1220 187 55 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 Functional -1905 45 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
150 2492 21 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 2492 21 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 2492 21 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 2492 21 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 2492 21 None 1 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
134 2497 24 3H-5HT -2 68 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-5HT -2 68 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-5HT -2 68 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-5HT -2 68 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-5HT -2 68 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
107 141 121 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 121 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -12 31 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
11154555 797 62 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 797 62 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 797 62 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 797 62 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 797 62 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 797 62 None -39 12 Human 8.0 pKi = 8.0 Binding
CHO-K1 cells, [3H]LSD (1.2nM)CHO-K1 cells, [3H]LSD (1.2nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2497 24 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 None -2 68 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cellsDisplacement of [3H]mesulergine from human HTR2B expressed in CHO-K1 cells
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
242 469 124 None -1 52 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 None -1 52 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 None -1 52 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 None -1 52 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 None -1 52 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
5 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135 2515 43 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 3H-5HT -3 58 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
46780481 107504 20 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107504 20 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107504 20 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107504 20 None -57 54 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
5 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -13 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
11848625 5760 0 UNDEFINED 2 6 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1078745 5760 0 UNDEFINED 2 6 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
62787 206165 21 3H-5HT -3 10 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 206165 21 3H-5HT -3 10 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
7153 97992 77 3H-KETANSERIN -50 34 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97992 77 3H-KETANSERIN -50 34 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
None 216000 0 3H-5HT -10 4 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216425 0 3H-5HT -43 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 419 6 1 4 3.4 C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCOC4=CC=C(C=C4)F.Cl None
10624 70271 19 3H-LSD -7 33 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 70271 19 3H-LSD -7 33 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 70271 19 3H-LSD -7 33 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
282 1407 0 None -371 7 Human 7.5 pKi = 7.5 Binding
Biased for β-arrestin signalling.Biased for β-arrestin signalling.
Guide to Pharmacology 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 23519215
522609 1407 0 None -371 7 Human 7.5 pKi = 7.5 Binding
Biased for β-arrestin signalling.Biased for β-arrestin signalling.
Guide to Pharmacology 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 23519215
1621 2413 17 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
17 2413 17 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
5761 2413 17 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
CHEMBL263881 2413 17 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
DB04829 2413 17 None -19 45 Human 8.4 pKi = 8.4 Binding
Biased for β-arrestin sihnalling.Biased for β-arrestin sihnalling.
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 23519215
10287037 623 0 None 31 2 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 3 0 4 5.1 CCOc1ccc2c(c1)Sc1c(C2=C2CCN(CC2)C)c(OC)ccc1 25666387
8424 623 0 None 31 2 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 367 3 0 4 5.1 CCOc1ccc2c(c1)Sc1c(C2=C2CCN(CC2)C)c(OC)ccc1 25666387
2 3237 23 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
2 3237 23 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 15322733
54562 3237 23 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
54562 3237 23 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 15322733
CHEMBL240773 3237 23 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
CHEMBL240773 3237 23 None -363 29 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 15322733
11658860 2329 51 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
2941 2329 51 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
4374 2329 51 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
CHEMBL360328 2329 51 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
DB04871 2329 51 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 18252809
45275554 3287 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
8427 3287 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
CHEMBL3544975 3287 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
DB12798 3287 0 None -6 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 9 3 6 3.7 COc1cc(N)c(cc1C(=O)NCC1CCN(CC1)CC[C@@H](c1ccc(cc1)F)OC(=O)N)Cl 25316608
11957541 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
11957541 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
1229 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
1229 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
147 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
147 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
170617 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
170617 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
CHEMBL6616 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
CHEMBL6616 1446 40 None -6 16 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8450835
11957541 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
11957541 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
11957541 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
1229 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
1229 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
1229 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
147 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
147 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
147 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
170617 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
170617 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
170617 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
CHEMBL6616 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 12970106
CHEMBL6616 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 8078486
CHEMBL6616 1446 40 None -2 16 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC 9933142
161 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 12970106
161 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15322733
161 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15466450
4284720 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 12970106
4284720 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15322733
4284720 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15466450
CHEMBL1255834 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 12970106
CHEMBL1255834 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15322733
CHEMBL1255834 751 6 None 2 6 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N 15466450
166 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 15322733
3045227 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 15322733
CHEMBL76781 3334 18 None 1 3 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 15322733
135 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
135 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
135 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
1796 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
1796 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
1796 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
4184 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
4184 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
4184 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
CHEMBL6437 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
CHEMBL6437 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
CHEMBL6437 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
DB06148 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10455251
DB06148 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 15322733
DB06148 2515 43 None -3 58 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9459568
134 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
134 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
134 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
1775 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
1775 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
1775 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
9681 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
9681 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
9681 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
CHEMBL1065 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
CHEMBL1065 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
CHEMBL1065 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
DB00247 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 11104741
DB00247 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 15322733
DB00247 2497 24 None -2 68 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9459568
176 1525 0 None 19 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 4 1 5 2.8 Nc1cc(N2CCN(CC2)Cc2ccccc2)c(cc1C)[N+](=O)[O-] 15107597
9930789 1525 0 None 19 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 4 1 5 2.8 Nc1cc(N2CCN(CC2)Cc2ccccc2)c(cc1C)[N+](=O)[O-] 15107597
CHEMBL1628720 1525 0 None 19 4 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 4 1 5 2.8 Nc1cc(N2CCN(CC2)Cc2ccccc2)c(cc1C)[N+](=O)[O-] 15107597
188 3366 80 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10455251
188 3366 80 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 15322733
196968 3366 80 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10455251
196968 3366 80 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 15322733
CHEMBL473186 3366 80 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10455251
CHEMBL473186 3366 80 None -1 6 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 15322733
3763 217685 0 None - 1 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 184 2 0 1 2.4 FC(F)OC(Cl)C(F)(F)F None
202 1496 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1496 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1496 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1496 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1496 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
3337 206344 27 None -75 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 None -75 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 None -75 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 None -75 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 None -75 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
4450 178204 69 None -1 3 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 None
CHEMBL465026 178204 69 None -1 3 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 None
6166 215998 0 None -4 4 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 330 2 1 3 3.7 C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)CO)CCC4=CC(=O)CC[C@]34C None
179 399 115 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 399 115 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 399 115 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 399 115 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 399 115 None -17 51 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
1357 2468 139 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
1672 2468 139 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
224 2468 139 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
896 2468 139 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
CHEMBL45 2468 139 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
DB01065 2468 139 None -3890 9 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12750432
1209 1645 75 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
203 1645 75 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
3386 1645 75 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
CHEMBL41 1645 75 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
DB00472 1645 75 None -199 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
208 2843 0 None -69 13 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
4541 2843 0 None -69 13 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
CHEMBL1494 2843 0 None -69 13 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 11104741
1220 187 55 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
1220 187 55 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
31 187 55 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
31 187 55 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
7 187 55 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
7 187 55 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
CHEMBL56 187 55 None -1905 45 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 15322733
CHEMBL56 187 55 None -3235 45 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450835
1524 2168 96 None -2691 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
197 2168 96 None -2691 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
3822 2168 96 None -2691 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
88 2168 96 None -2691 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
CHEMBL51 2168 96 None -2691 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
DB12465 2168 96 None -2691 52 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8450835
186 1794 52 None -426 17 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 15322733
71781 1794 52 None -426 17 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 15322733
CHEMBL18972 1794 52 None -426 17 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 15322733
2470 3626 50 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
3300 3626 50 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
5265 3626 50 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
99 3626 50 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
CHEMBL267930 3626 50 None -120226 60 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8450835
2176 3104 68 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
4828 3104 68 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
91 3104 68 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
CHEMBL500 3104 68 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
DB00960 3104 68 None -933 27 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 15322733
29 789 0 None -2511 9 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
9805719 789 0 None -2511 9 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
CHEMBL2027925 789 0 None -2511 9 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
18971832 2402 0 None -263 13 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
21 2402 0 None -263 13 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
CHEMBL3186179 2402 0 None -263 13 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
28 3470 46 None -954 10 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
3292447 3470 46 None -954 10 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL20963 3470 46 None -954 10 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
2202 3110 96 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 3110 96 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 3110 96 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 3110 96 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 3110 96 None -6 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
130 3474 47 None -478 13 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 15322733
3378093 3474 47 None -478 13 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 15322733
CHEMBL281350 3474 47 None -478 13 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 15322733
143 3489 51 None -158 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10945872
5311096 3489 51 None -158 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10945872
CHEMBL85606 3489 51 None -158 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10945872
175 3628 44 None -331 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
68186 3628 44 None -331 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
CHEMBL79834 3628 44 None -331 7 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
185 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
185 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
5311271 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
5311271 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
CHEMBL74355 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
CHEMBL74355 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
DB16351 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10188965
DB16351 3975 60 None -2344 38 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 15322733
187 3363 18 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 15322733
187 3363 18 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 9225287
3693566 3363 18 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 15322733
3693566 3363 18 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 9225287
CHEMBL88402 3363 18 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 15322733
CHEMBL88402 3363 18 None -288 5 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 3 8 3.6 COc1cc(OC)c(cc1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O)NS(=O)(=O)c1ccc(cc1)C(F)(F)F 9225287
1353 1898 93 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
3559 1898 93 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
86 1898 93 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
CHEMBL54 1898 93 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
DB00502 1898 93 None -295 86 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 9459568
109 899 31 None -281 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 15322733
2689 899 31 None -281 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 15322733
CHEMBL27403 899 31 None -281 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 15322733
2470 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
2470 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
2470 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
3300 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
3300 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
3300 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
5265 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
5265 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
5265 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
99 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
99 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
99 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
CHEMBL267930 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 15322733
CHEMBL267930 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8078486
CHEMBL267930 3626 50 None -14125 60 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 9459568
107780 1831 54 None -676 18 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
14 1831 54 None -676 18 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL15928 1831 54 None -676 18 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
133633 2228 53 None -87 8 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10869410
177 2228 53 None -87 8 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10869410
CHEMBL445102 2228 53 None -87 8 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10869410
177336 3098 50 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
225 3098 50 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
CHEMBL356359 3098 50 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
DB04873 3098 50 None -1412 3 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 11504648
1524 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
1524 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
1524 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
1524 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
1524 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
197 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
197 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
197 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
197 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
197 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
3822 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
3822 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
3822 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
3822 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
3822 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
88 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
88 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
88 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
88 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
88 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
CHEMBL51 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
CHEMBL51 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
CHEMBL51 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
CHEMBL51 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
CHEMBL51 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
DB12465 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 12738034
DB12465 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 15322733
DB12465 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8078486
DB12465 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 8845011
DB12465 2168 96 None -229 52 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9459568
107992 2536 49 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
165 2536 49 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
CHEMBL269521 2536 49 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
DB12111 2536 49 None -5 10 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 8450835
107992 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
107992 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
165 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
165 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
CHEMBL269521 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
CHEMBL269521 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
DB12111 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 12970106
DB12111 2536 49 None -1 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 15322733
5268 3629 40 None -1047 18 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 9459568
53 3629 40 None -1047 18 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 9459568
CHEMBL300555 3629 40 None -1047 18 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 9459568
1574 81 60 None -3 21 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 8450835
218 81 60 None -3 21 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 8450835
CHEMBL266591 81 60 None -3 21 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 8450835
198 312 126 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
82148 312 126 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
99 312 126 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
CHEMBL10878 312 126 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
DB06594 312 126 None -346 6 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12750432
177336 3098 50 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
225 3098 50 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
CHEMBL356359 3098 50 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
DB04873 3098 50 None -1412 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 4 3.7 CCCCN1CCC(CC1)CNC(=O)c1c2OCCCn2c2c1cccc2 15466450
210 3451 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
2423 3451 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
5160 3451 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
CHEMBL52939 3451 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
DB12163 3451 0 None -7 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 429 13 1 6 3.2 COc1cccc(c1)CCc1ccccc1OCC(OC(=O)CCC(=O)O)CN(C)C 12738034
195 3544 7 None -25 4 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 0 0 2 2.1 CN1CC[C@H]2[C@@H](C1)c1cccc3c1N(C2)CC3 15322733
9859407 3544 7 None -25 4 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 0 0 2 2.1 CN1CC[C@H]2[C@@H](C1)c1cccc3c1N(C2)CC3 15322733
CHEMBL316069 3544 7 None -25 4 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 0 0 2 2.1 CN1CC[C@H]2[C@@H](C1)c1cccc3c1N(C2)CC3 15322733
1809 134 32 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 15322733
1809 134 32 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
4 134 32 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 15322733
4 134 32 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
CHEMBL18840 134 32 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 15322733
CHEMBL18840 134 32 None -999 37 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
1809 134 32 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
1809 134 32 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450835
4 134 32 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
4 134 32 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450835
CHEMBL18840 134 32 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8078486
CHEMBL18840 134 32 None -1659 37 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450835
129 3414 10 None -562 9 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
9868452 3414 10 None -562 9 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
CHEMBL65280 3414 10 None -562 9 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
193 3480 46 None -707 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 15322733
193 3480 46 None -707 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 9225286
3644637 3480 46 None -707 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 15322733
3644637 3480 46 None -707 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 9225286
CHEMBL14563 3480 46 None -707 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 15322733
CHEMBL14563 3480 46 None -707 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 3 1 4 5.1 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1ccc(nc1)Oc1cccnc1C 9225286
228 444 28 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 444 28 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 444 28 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 444 28 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 444 28 None -5 24 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
173 3238 95 None -3 23 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 8450835
5011 3238 95 None -3 23 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 8450835
CHEMBL18772 3238 95 None -3 23 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 8450835
108029 3389 57 None -125 13 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 15322733
23 3389 57 None -125 13 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 15322733
CHEMBL18785 3389 57 None -125 13 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 15322733
221 3465 71 None -4 14 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 15322733
3277600 3465 71 None -4 14 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 15322733
CHEMBL323356 3465 71 None -4 14 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C 15322733
170 2941 0 None -6 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 1 1 3 2.2 FC(c1ccc(nc1Cl)N1CCNCC1)(F)F 15322733
9796408 2941 0 None -6 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 1 1 3 2.2 FC(c1ccc(nc1Cl)N1CCNCC1)(F)F 15322733
CHEMBL506999 2941 0 None -6 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 1 1 3 2.2 FC(c1ccc(nc1Cl)N1CCNCC1)(F)F 15322733
194 3481 31 None -100 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10737744
443391 3481 31 None -100 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10737744
CHEMBL14460 3481 31 None -100 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10737744
1150 3849 121 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
1150 3849 121 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
125 3849 121 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
125 3849 121 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
CHEMBL6640 3849 121 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
CHEMBL6640 3849 121 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
DB08653 3849 121 None -2 25 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 15322733
DB08653 3849 121 None -8 25 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 8450835
173 3238 95 None 1 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 15322733
5011 3238 95 None 1 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 15322733
CHEMBL18772 3238 95 None 1 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 15322733
115 3762 80 None -2 27 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450835
4296 3762 80 None -2 27 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450835
CHEMBL274866 3762 80 None -2 27 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450835
213 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
213 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
2717 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
2717 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
5533 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
5533 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
CHEMBL621 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
CHEMBL621 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
DB00656 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 11104741
DB00656 3824 55 None -5 44 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 15322733
115 3762 80 None -1 27 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 15322733
4296 3762 80 None -1 27 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 15322733
CHEMBL274866 3762 80 None -1 27 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 15322733
31101 726 40 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 726 40 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 726 40 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 726 40 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 726 40 None -26 36 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
135 2515 43 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
1796 2515 43 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
4184 2515 43 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
CHEMBL6437 2515 43 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
DB06148 2515 43 None -37 58 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8450835
15897 2840 0 None 12 37 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N 11104741
215 2840 0 None 12 37 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N 11104741
CHEMBL1979333 2840 0 None 12 37 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N 11104741
12895728 2841 0 None - 1 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@H](Cc1cccc(c1)C(F)(F)F)N 11104741
217 2841 0 None - 1 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@H](Cc1cccc(c1)C(F)(F)F)N 11104741
CHEMBL250881 2841 0 None - 1 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@H](Cc1cccc(c1)C(F)(F)F)N 11104741
102 4096 48 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
3659 4096 48 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
8969 4096 48 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
CHEMBL15245 4096 48 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
DB01392 4096 48 None -100 50 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
157 2056 7 None -20 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 15322733
157 2056 7 None -20 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 9857084
9840090 2056 7 None -20 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 15322733
9840090 2056 7 None -20 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 9857084
CHEMBL134519 2056 7 None -20 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 15322733
CHEMBL134519 2056 7 None -20 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 9857084
10 720 28 None -3 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3654103 720 28 None -3 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
CHEMBL534232 720 28 None -3 9 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
206 2476 16 None -26 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8450835
68848 2476 16 None -26 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8450835
CHEMBL12314 2476 16 None -26 25 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8450835
171 2943 0 None -5 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 233 3 1 3 1.9 COc1ccc2c(c1O[C@@H]1CNCC1)CCC2 15322733
9794656 2943 0 None -5 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 233 3 1 3 1.9 COc1ccc2c(c1O[C@@H]1CNCC1)CCC2 15322733
136 3267 32 None -63 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
223 3267 32 None -63 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
643606 3267 32 None -63 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
CHEMBL10347 3267 32 None -63 16 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450835
155 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
155 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
163 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
163 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
62065 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
62065 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
CHEMBL6607 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
CHEMBL6607 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
DB01484 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 15322733
DB01484 725 25 None -5 13 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC 9933142
219050 3348 25 None -194 21 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 3348 25 None -194 21 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 3348 25 None -194 21 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
168 3951 15 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 15322733
6604042 3951 15 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 15322733
CHEMBL309760 3951 15 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 2 1 2 2.2 C[C@@H](CN1CCc2c1cc(Br)cc2)N 15322733
153 1447 9 None -25 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@@H](N)C)OC 15322733
6603801 1447 9 None -25 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@@H](N)C)OC 15322733
CHEMBL1434583 1447 9 None -25 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@@H](N)C)OC 15322733
1355 1998 88 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
142 1998 88 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
CHEMBL478 1998 88 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
DB12110 1998 88 None -1 16 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 8450835
102 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
102 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
102 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
3659 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
3659 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
3659 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
8969 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
8969 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
8969 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
CHEMBL15245 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
CHEMBL15245 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
CHEMBL15245 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
DB01392 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10455251
DB01392 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8078486
DB01392 4096 48 None -93 50 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
157 2056 7 None -20 4 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 12954071
9840090 2056 7 None -20 4 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 12954071
CHEMBL134519 2056 7 None -20 4 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 4 1 3 2.2 COc1cc(I)c(cc1C[C@H](N)C)OC 12954071
3652 4066 79 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4066 79 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4066 79 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4066 79 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4066 79 None -2 18 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
108029 3389 57 None -15 13 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450835
23 3389 57 None -15 13 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450835
CHEMBL18785 3389 57 None -15 13 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450835
13878025 2411 0 None -19 3 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 3 2 4 2.4 CC(C(OC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C)O 8450835
184 2411 0 None -19 3 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 3 2 4 2.4 CC(C(OC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C)O 8450835
CHEMBL52422 2411 0 None -19 3 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 3 2 4 2.4 CC(C(OC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C)O 8450835
1355 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
1355 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
1355 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
1355 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
1355 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
142 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
142 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
142 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
142 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
142 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
CHEMBL478 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
CHEMBL478 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
CHEMBL478 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
CHEMBL478 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
CHEMBL478 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
DB12110 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 11104741
DB12110 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 12970106
DB12110 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 15322733
DB12110 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9459568
DB12110 1998 88 None -1 16 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 9933142
5 139 72 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
5202 139 72 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
CHEMBL39 139 72 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
DB08839 139 72 None -29 55 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450835
107 141 121 None -12 31 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8450835
1833 141 121 None -12 31 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8450835
CHEMBL8165 141 121 None -12 31 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8450835
152 363 29 None -1 19 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8450835
2107 363 29 None -1 19 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8450835
CHEMBL275854 363 29 None -1 19 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8450835
199 391 0 None -5 5 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 8450835
9821951 391 0 None -5 5 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 8450835
CHEMBL160293 391 0 None -5 5 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 3 4.6 O=C([C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C)NC1CCCCC1 8450835
216 2842 32 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 11104741
9815618 2842 32 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 11104741
CHEMBL253811 2842 32 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 11104741
189 3466 39 None -5 17 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15322733
189 3466 39 None -5 17 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15466450
5163 3466 39 None -5 17 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15322733
5163 3466 39 None -5 17 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15466450
CHEMBL297784 3466 39 None -5 17 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15322733
CHEMBL297784 3466 39 None -5 17 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 15466450
192 3476 54 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10188965
192 3476 54 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10737744
443390 3476 54 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10188965
443390 3476 54 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10737744
CHEMBL14276 3476 54 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10188965
CHEMBL14276 3476 54 None -10 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 3 1 3 5.5 COc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cc(F)cc(c1)c1cccnc1 10737744
136 3267 32 None -8 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
223 3267 32 None -8 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
643606 3267 32 None -8 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
CHEMBL10347 3267 32 None -8 16 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 9459568
152 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15322733
152 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
152 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8078486
2107 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15322733
2107 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
2107 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8078486
CHEMBL275854 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15322733
CHEMBL275854 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 15466450
CHEMBL275854 363 29 None 1 19 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 8078486
5 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
5 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
5 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
5 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
5 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
5202 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
5202 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
5202 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
5202 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
5202 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
CHEMBL39 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
CHEMBL39 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
CHEMBL39 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
CHEMBL39 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
CHEMBL39 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
DB08839 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11104741
DB08839 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 12954071
DB08839 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15322733
DB08839 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 15466450
DB08839 139 72 None -13 55 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8078486
183 2409 0 None -5 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 8450835
3034814 2409 0 None -5 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 8450835
CHEMBL1356280 2409 0 None -5 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 8450835
133 2479 52 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
1723 2479 52 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
28693 2479 52 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
CHEMBL19215 2479 52 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
DB13520 2479 52 None -12 43 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8450835
134 2497 24 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
1775 2497 24 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
9681 2497 24 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
CHEMBL1065 2497 24 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
DB00247 2497 24 None -12 68 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450835
2105 3032 37 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 3032 37 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 3032 37 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 3032 37 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 3032 37 None -28 33 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
2601 3751 33 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
443951 3751 33 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
56 3751 33 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL73151 3751 33 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB13399 3751 33 None -8 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
10331436 323 10 None -2 6 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 12954071
160 323 10 None -2 6 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 12954071
CHEMBL133455 323 10 None -2 6 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 12954071
1621 2413 17 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
17 2413 17 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
5761 2413 17 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
CHEMBL263881 2413 17 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
DB04829 2413 17 None -39 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12213075
5074 3307 80 None -8 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
97 3307 80 None -8 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
CHEMBL267777 3307 80 None -8 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
DB12693 3307 80 None -8 30 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8450835
10449757 3469 35 None 3 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10188965
190 3469 35 None 3 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10188965
CHEMBL2110371 3469 35 None 3 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 1 1 2 4.8 O=C(N1CCc2c1cc(Cl)c(c2)C)Nc1cccc2c1cccn2 10188965
1342 36 49 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
1342 36 49 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8450835
3 36 49 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
3 36 49 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8450835
CHEMBL277120 36 49 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
CHEMBL277120 36 49 None -4 19 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8450835
135398737 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
135398737 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
135398737 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
38 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
38 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
38 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
722 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
722 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
722 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
CHEMBL42 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
CHEMBL42 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
CHEMBL42 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
DB00363 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15322733
DB00363 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9459568
DB00363 955 93 None -2 92 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
167 3405 0 None -3 5 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
9821498 3405 0 None -3 5 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
135409453 3744 41 None 2 2 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
226 3744 41 None 2 2 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
CHEMBL76370 3744 41 None 2 2 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 15466450
191 3472 52 None -1 3 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 15322733
443389 3472 52 None -1 3 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 15322733
CHEMBL276140 3472 52 None -1 3 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 4.4 CSc1cc2CCN(c2cc1C(F)(F)F)C(=O)Nc1cccnc1 15322733
206 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15107597
206 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15322733
206 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9459568
68848 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15107597
68848 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15322733
68848 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9459568
CHEMBL12314 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15107597
CHEMBL12314 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 15322733
CHEMBL12314 2476 16 None -1 25 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9459568
1342 36 49 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
1342 36 49 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9459568
3 36 49 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
3 36 49 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9459568
CHEMBL277120 36 49 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8078486
CHEMBL277120 36 49 None 2 19 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9459568
1043 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11104741
1043 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 15322733
149 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11104741
149 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 15322733
8223 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11104741
8223 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 15322733
CHEMBL442 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11104741
CHEMBL442 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 15322733
DB00696 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11104741
DB00696 1569 14 None -22 29 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 15322733
133 2479 52 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
1723 2479 52 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
28693 2479 52 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
CHEMBL19215 2479 52 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
DB13520 2479 52 None -2 43 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 15322733
37 775 60 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 775 60 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 775 60 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 775 60 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 775 60 None 1 17 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
1588 2311 27 None -6 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 2311 27 None -6 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 2311 27 None -6 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 2311 27 None -6 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 2311 27 None -6 44 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
4106 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
4106 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
5358812 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
5358812 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
89 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
89 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
CHEMBL93240 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 15322733
CHEMBL93240 2485 22 None -3 34 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9459568
5074 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
5074 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
5074 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
5074 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
97 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
97 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
97 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
97 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
CHEMBL267777 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
CHEMBL267777 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
CHEMBL267777 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
CHEMBL267777 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
DB12693 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10188965
DB12693 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10455251
DB12693 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 15322733
DB12693 3307 80 None -2 30 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9459568
183 2409 0 None 2 4 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 9459568
3034814 2409 0 None 2 4 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 9459568
CHEMBL1356280 2409 0 None 2 4 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 4 1 5 3.5 CC(C(O)C)OC(=O)[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C(C)C 9459568
154 2344 0 None -1 4 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 15322733
638252 2344 0 None -1 4 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 15322733
150 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
150 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
1764 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
1764 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
8226 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
8226 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
CHEMBL1201356 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
CHEMBL1201356 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733
DB00353 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 11104741
DB00353 2492 21 None 1 16 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 15322733