Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

3036780 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3036780.0 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
46780481 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
9903970.0 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
CHEMBL504548 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB06216 107587 None 16 Human Functional pAC50 = 8.9 8.9 -6 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1462 None 65 Human Functional pAC50 = 5 5.0 -1905 24
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3151.0 1462 None 65 Human Functional pAC50 = 5 5.0 -1905 24
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1462 None 65 Human Functional pAC50 = 5 5.0 -1905 24
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1462 None 65 Human Functional pAC50 = 5 5.0 -1905 24
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1462 None 65 Human Functional pAC50 = 5 5.0 -1905 24
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1462 None 65 Human Functional pAC50 = 5 5.0 -1905 24
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 23803 None 71 Human Functional pAC50 = 5 5.0 -5 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 23803 None 71 Human Functional pAC50 = 5 5.0 -5 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 23803 None 71 Human Functional pAC50 = 5 5.0 -5 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 49659 None 55 Human Functional pAC50 = 5 5.0 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 49659 None 55 Human Functional pAC50 = 5 5.0 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78221 None 44 Human Functional pAC50 = 5 5.0 -3 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78221 None 44 Human Functional pAC50 = 5 5.0 -3 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 16653 None 45 Human Functional pAC50 = 5 5.0 -5 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 16653 None 45 Human Functional pAC50 = 5 5.0 -5 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 120083 None 57 Human Functional pAC50 = 5 5.0 -25 9
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 120083 None 57 Human Functional pAC50 = 5 5.0 -25 9
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 120083 None 57 Human Functional pAC50 = 5 5.0 -25 9
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 78293 None 10 Human Functional pAC50 = 6 6.0 -1 4
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 78293 None 10 Human Functional pAC50 = 6 6.0 -1 4
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
242 470 None 70 Human Functional pAC50 = 7.0 7.0 -33 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
34 470 None 70 Human Functional pAC50 = 7.0 7.0 -33 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 470 None 70 Human Functional pAC50 = 7.0 7.0 -33 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
60795.0 470 None 70 Human Functional pAC50 = 7.0 7.0 -33 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 470 None 70 Human Functional pAC50 = 7.0 7.0 -33 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 470 None 70 Human Functional pAC50 = 7.0 7.0 -33 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 352 None 46 Human Functional pAC50 = 5.0 5.0 -199 6
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
123606.0 352 None 46 Human Functional pAC50 = 5.0 5.0 -199 6
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
128 352 None 46 Human Functional pAC50 = 5.0 5.0 -199 6
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 352 None 46 Human Functional pAC50 = 5.0 5.0 -199 6
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 352 None 46 Human Functional pAC50 = 5.0 5.0 -199 6
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 352 None 46 Human Functional pAC50 = 5.0 5.0 -199 6
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 4643 None 51 Human Functional pAC50 = 5.0 5.0 -3 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4643 None 51 Human Functional pAC50 = 5.0 5.0 -3 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.0 5.0 -81 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.0 5.0 -81 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.0 5.0 -81 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.0 5.0 -81 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 12618 None 11 Human Functional pAC50 = 5.0 5.0 -30 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 12618 None 11 Human Functional pAC50 = 5.0 5.0 -30 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 31564 None 60 Human Functional pAC50 = 5.0 5.0 -7 9
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 31564 None 60 Human Functional pAC50 = 5.0 5.0 -7 9
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 31564 None 60 Human Functional pAC50 = 5.0 5.0 -7 9
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 55838 None 37 Human Functional pAC50 = 5.0 5.0 -8 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4034.0 55838 None 37 Human Functional pAC50 = 5.0 5.0 -8 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 55838 None 37 Human Functional pAC50 = 5.0 5.0 -8 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB00737 55838 None 37 Human Functional pAC50 = 5.0 5.0 -8 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 106495 None 32 Human Functional pAC50 = 5.0 5.0 -1548 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 106495 None 32 Human Functional pAC50 = 5.0 5.0 -1548 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
180 401 None 38 Human Functional pAC50 = 6.0 6.0 -398 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
200 401 None 38 Human Functional pAC50 = 6.0 6.0 -398 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 401 None 38 Human Functional pAC50 = 6.0 6.0 -398 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2160.0 401 None 38 Human Functional pAC50 = 6.0 6.0 -398 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 401 None 38 Human Functional pAC50 = 6.0 6.0 -398 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 401 None 38 Human Functional pAC50 = 6.0 6.0 -398 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2759 None 31 Human Functional pAC50 = 6.0 6.0 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2759 None 31 Human Functional pAC50 = 6.0 6.0 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2759 None 31 Human Functional pAC50 = 6.0 6.0 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2759 None 31 Human Functional pAC50 = 6.0 6.0 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2759 None 31 Human Functional pAC50 = 6.0 6.0 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 31768 None 42 Human Functional pAC50 = 6.0 6.0 17 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 31768 None 42 Human Functional pAC50 = 6.0 6.0 17 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 122423 None 61 Human Functional pAC50 = 5.0 5.0 -5 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 122423 None 61 Human Functional pAC50 = 5.0 5.0 -5 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 19421 None 48 Human Functional pAC50 = 5.9 5.9 1 11
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 19421 None 48 Human Functional pAC50 = 5.9 5.9 1 11
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 4107 None 38 Human Functional pAC50 = 5.9 5.9 -141 18
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 4107 None 38 Human Functional pAC50 = 5.9 5.9 -141 18
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 4107 None 38 Human Functional pAC50 = 5.9 5.9 -141 18
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
5709.0 4107 None 38 Human Functional pAC50 = 5.9 5.9 -141 18
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 4107 None 38 Human Functional pAC50 = 5.9 5.9 -141 18
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 4107 None 38 Human Functional pAC50 = 5.9 5.9 -141 18
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
191 403 None 60 Human Functional pAC50 = 6.9 6.9 -3 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
201 403 None 60 Human Functional pAC50 = 6.9 6.9 -3 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 403 None 60 Human Functional pAC50 = 6.9 6.9 -3 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2170.0 403 None 60 Human Functional pAC50 = 6.9 6.9 -3 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 403 None 60 Human Functional pAC50 = 6.9 6.9 -3 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 403 None 60 Human Functional pAC50 = 6.9 6.9 -3 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2348 None 42 Human Functional pAC50 = 6.9 6.9 -3 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2348 None 42 Human Functional pAC50 = 6.9 6.9 -3 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2348 None 42 Human Functional pAC50 = 6.9 6.9 -3 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3964.0 2348 None 42 Human Functional pAC50 = 6.9 6.9 -3 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2348 None 42 Human Functional pAC50 = 6.9 6.9 -3 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2348 None 42 Human Functional pAC50 = 6.9 6.9 -3 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78295 None 23 Human Functional pAC50 = 6.9 6.9 1 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78295 None 23 Human Functional pAC50 = 6.9 6.9 1 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 56283 None 21 Human Functional pAC50 = 5.9 5.9 -323 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3158.0 56283 None 21 Human Functional pAC50 = 5.9 5.9 -323 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 56283 None 21 Human Functional pAC50 = 5.9 5.9 -323 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB01142 56283 None 21 Human Functional pAC50 = 5.9 5.9 -323 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 82440 None 34 Human Functional pAC50 = 5.9 5.9 -75 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 82440 None 34 Human Functional pAC50 = 5.9 5.9 -75 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206466 None 47 Human Functional pAC50 = 5.9 5.9 -1 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206466 None 47 Human Functional pAC50 = 5.9 5.9 -1 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206466 None 47 Human Functional pAC50 = 5.9 5.9 -1 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14501 None 15 Human Functional pAC50 = 4.9 4.9 1 4
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
5906.0 14501 None 15 Human Functional pAC50 = 4.9 4.9 1 4
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 14501 None 15 Human Functional pAC50 = 4.9 4.9 1 4
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
DB00610 14501 None 15 Human Functional pAC50 = 4.9 4.9 1 4
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 35070 None 5 Human Functional pAC50 = 4.9 4.9 -2 28
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 35070 None 5 Human Functional pAC50 = 4.9 4.9 -2 28
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 35070 None 5 Human Functional pAC50 = 4.9 4.9 -2 28
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 207349 None 24 Human Functional pAC50 = 4.9 4.9 -10 19
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 207349 None 24 Human Functional pAC50 = 4.9 4.9 -10 19
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 207349 None 24 Human Functional pAC50 = 4.9 4.9 -10 19
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 25 None 53 Human Functional pAC50 = 4.9 4.9 -7079 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 25 None 53 Human Functional pAC50 = 4.9 4.9 -7079 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 25 None 53 Human Functional pAC50 = 4.9 4.9 -7079 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 25 None 53 Human Functional pAC50 = 4.9 4.9 -7079 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 25 None 53 Human Functional pAC50 = 4.9 4.9 -7079 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 25 None 53 Human Functional pAC50 = 4.9 4.9 -7079 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1432 None 51 Human Functional pAC50 = 4.9 4.9 -707 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1432 None 51 Human Functional pAC50 = 4.9 4.9 -707 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3100.0 1432 None 51 Human Functional pAC50 = 4.9 4.9 -707 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1432 None 51 Human Functional pAC50 = 4.9 4.9 -707 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1432 None 51 Human Functional pAC50 = 4.9 4.9 -707 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1432 None 51 Human Functional pAC50 = 4.9 4.9 -707 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1432 None 51 Human Functional pAC50 = 4.9 4.9 -707 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1508 None 46 Human Functional pAC50 = 4.9 4.9 -8 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1508 None 46 Human Functional pAC50 = 4.9 4.9 -8 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1508 None 46 Human Functional pAC50 = 4.9 4.9 -8 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1508 None 46 Human Functional pAC50 = 4.9 4.9 -8 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1508 None 46 Human Functional pAC50 = 4.9 4.9 -8 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3463 None 53 Human Functional pAC50 = 4.9 4.9 -21379 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3463 None 53 Human Functional pAC50 = 4.9 4.9 -21379 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5152.0 3463 None 53 Human Functional pAC50 = 4.9 4.9 -21379 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3463 None 53 Human Functional pAC50 = 4.9 4.9 -21379 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3463 None 53 Human Functional pAC50 = 4.9 4.9 -21379 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3463 None 53 Human Functional pAC50 = 4.9 4.9 -21379 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3578 None 61 Human Functional pAC50 = 4.9 4.9 -457 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3578 None 61 Human Functional pAC50 = 4.9 4.9 -457 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3578 None 61 Human Functional pAC50 = 4.9 4.9 -457 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
9913767.0 3578 None 61 Human Functional pAC50 = 4.9 4.9 -457 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3578 None 61 Human Functional pAC50 = 4.9 4.9 -457 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3578 None 61 Human Functional pAC50 = 4.9 4.9 -457 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4132 None 63 Human Functional pAC50 = 4.9 4.9 -6025 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4132 None 63 Human Functional pAC50 = 4.9 4.9 -6025 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4132 None 63 Human Functional pAC50 = 4.9 4.9 -6025 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5717.0 4132 None 63 Human Functional pAC50 = 4.9 4.9 -6025 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4132 None 63 Human Functional pAC50 = 4.9 4.9 -6025 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4132 None 63 Human Functional pAC50 = 4.9 4.9 -6025 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 15552 None 54 Human Functional pAC50 = 4.9 4.9 -6 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 15552 None 54 Human Functional pAC50 = 4.9 4.9 -6 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 41527 None 58 Human Functional pAC50 = 4.9 4.9 -6 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 41527 None 58 Human Functional pAC50 = 4.9 4.9 -6 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 172649 None 27 Human Functional pAC50 = 4.9 4.9 -7 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 172649 None 27 Human Functional pAC50 = 4.9 4.9 -7 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 15305 None 29 Human Functional pAC50 = 4.9 4.9 -6 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 15305 None 29 Human Functional pAC50 = 4.9 4.9 -6 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 15305 None 29 Human Functional pAC50 = 4.9 4.9 -6 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206050 None 27 Human Functional pAC50 = 5.9 5.9 -60 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2895.0 206050 None 27 Human Functional pAC50 = 5.9 5.9 -60 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206050 None 27 Human Functional pAC50 = 5.9 5.9 -60 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB00924 206050 None 27 Human Functional pAC50 = 5.9 5.9 -60 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.9 5.9 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.9 5.9 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.9 5.9 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.9 5.9 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.9 5.9 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.9 5.9 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.9 5.9 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3707 None 46 Human Functional pAC50 = 4.9 4.9 -1023 14
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 3707 None 46 Human Functional pAC50 = 4.9 4.9 -1023 14
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
5358.0 3707 None 46 Human Functional pAC50 = 4.9 4.9 -1023 14
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 3707 None 46 Human Functional pAC50 = 4.9 4.9 -1023 14
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 3707 None 46 Human Functional pAC50 = 4.9 4.9 -1023 14
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 3707 None 46 Human Functional pAC50 = 4.9 4.9 -1023 14
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 206828 None 60 Human Functional pAC50 = 4.9 4.9 -11 8
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 206828 None 60 Human Functional pAC50 = 4.9 4.9 -11 8
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 98790 None 31 Human Functional pAC50 = 5.9 5.9 -117 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98790 None 31 Human Functional pAC50 = 5.9 5.9 -117 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 102785 None 36 Human Functional pAC50 = 5.9 5.9 -208 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
16351.0 102785 None 36 Human Functional pAC50 = 5.9 5.9 -208 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 102785 None 36 Human Functional pAC50 = 5.9 5.9 -208 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB13256 102785 None 36 Human Functional pAC50 = 5.9 5.9 -208 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 18873 None 78 Human Functional pAC50 = 4.9 4.9 -10 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 18873 None 78 Human Functional pAC50 = 4.9 4.9 -10 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3183 None 36 Human Functional pAC50 = 5.9 5.9 -40 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3183 None 36 Human Functional pAC50 = 5.9 5.9 -40 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4927.0 3183 None 36 Human Functional pAC50 = 5.9 5.9 -40 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3183 None 36 Human Functional pAC50 = 5.9 5.9 -40 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3183 None 36 Human Functional pAC50 = 5.9 5.9 -40 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3183 None 36 Human Functional pAC50 = 5.9 5.9 -40 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3334 None 46 Human Functional pAC50 = 4.9 4.9 -1096 8
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 3334 None 46 Human Functional pAC50 = 4.9 4.9 -1096 8
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
5078.0 3334 None 46 Human Functional pAC50 = 4.9 4.9 -1096 8
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 3334 None 46 Human Functional pAC50 = 4.9 4.9 -1096 8
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 3334 None 46 Human Functional pAC50 = 4.9 4.9 -1096 8
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 3334 None 46 Human Functional pAC50 = 4.9 4.9 -1096 8
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 2483 None 21 Human Functional pAC50 = 4.9 4.9 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2483 None 21 Human Functional pAC50 = 4.9 4.9 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2483 None 21 Human Functional pAC50 = 4.9 4.9 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2483 None 21 Human Functional pAC50 = 4.9 4.9 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1288 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1288 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1288 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1288 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3330 None 58 Human Functional pAC50 = 4.9 4.9 -1288 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3371 None 67 Human Functional pAC50 = 4.9 4.9 -25 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3371 None 67 Human Functional pAC50 = 4.9 4.9 -25 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3371 None 67 Human Functional pAC50 = 4.9 4.9 -25 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3371 None 67 Human Functional pAC50 = 4.9 4.9 -25 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3371 None 67 Human Functional pAC50 = 4.9 4.9 -25 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3997 None 65 Human Functional pAC50 = 4.9 4.9 -1778 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
24776445.0 3997 None 65 Human Functional pAC50 = 4.9 4.9 -1778 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3997 None 65 Human Functional pAC50 = 4.9 4.9 -1778 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3997 None 65 Human Functional pAC50 = 4.9 4.9 -1778 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3997 None 65 Human Functional pAC50 = 4.9 4.9 -1778 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3997 None 65 Human Functional pAC50 = 4.9 4.9 -1778 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 93987 None 66 Human Functional pAC50 = 4.9 4.9 -22 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 93987 None 66 Human Functional pAC50 = 4.9 4.9 -22 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 106524 None 30 Human Functional pAC50 = 4.9 4.9 -537 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 106524 None 30 Human Functional pAC50 = 4.9 4.9 -537 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 111768 None 45 Human Functional pAC50 = 4.9 4.9 -11 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 111768 None 45 Human Functional pAC50 = 4.9 4.9 -11 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 17965 None 17 Human Functional pAC50 = 4.8 4.8 -12 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 17965 None 17 Human Functional pAC50 = 4.8 4.8 -12 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189074 None 0 Human Functional pAC50 = 4.8 4.8 -218 15
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 3054 None 28 Human Functional pAC50 = 7.8 7.8 -3 25
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 3054 None 28 Human Functional pAC50 = 7.8 7.8 -3 25
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 3054 None 28 Human Functional pAC50 = 7.8 7.8 -3 25
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 3054 None 28 Human Functional pAC50 = 7.8 7.8 -3 25
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 3054 None 28 Human Functional pAC50 = 7.8 7.8 -3 25
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 2344 None 24 Human Functional pAC50 = 6.8 6.8 -35 11
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 2344 None 24 Human Functional pAC50 = 6.8 6.8 -35 11
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 2344 None 24 Human Functional pAC50 = 6.8 6.8 -35 11
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 2344 None 24 Human Functional pAC50 = 6.8 6.8 -35 11
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 2344 None 24 Human Functional pAC50 = 6.8 6.8 -35 11
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 1389 None 72 Human Functional pAC50 = 6.8 6.8 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
124087.0 1389 None 72 Human Functional pAC50 = 6.8 6.8 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1389 None 72 Human Functional pAC50 = 6.8 6.8 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1389 None 72 Human Functional pAC50 = 6.8 6.8 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1389 None 72 Human Functional pAC50 = 6.8 6.8 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1389 None 72 Human Functional pAC50 = 6.8 6.8 -1 27
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206241 None 47 Human Functional pAC50 = 5.8 5.8 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206241 None 47 Human Functional pAC50 = 5.8 5.8 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206241 None 47 Human Functional pAC50 = 5.8 5.8 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 209745 None 64 Human Functional pAC50 = 4.8 4.8 -7 7
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 209745 None 64 Human Functional pAC50 = 4.8 4.8 -7 7
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 1658 None 52 Human Functional pAC50 = 4.8 4.8 -56 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1658 None 52 Human Functional pAC50 = 4.8 4.8 -56 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1658 None 52 Human Functional pAC50 = 4.8 4.8 -56 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1658 None 52 Human Functional pAC50 = 4.8 4.8 -56 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1658 None 52 Human Functional pAC50 = 4.8 4.8 -56 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3869 None 33 Human Functional pAC50 = 4.8 4.8 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3869 None 33 Human Functional pAC50 = 4.8 4.8 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3869 None 33 Human Functional pAC50 = 4.8 4.8 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3869 None 33 Human Functional pAC50 = 4.8 4.8 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3869 None 33 Human Functional pAC50 = 4.8 4.8 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 34413 None 64 Human Functional pAC50 = 4.8 4.8 -9 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 34413 None 64 Human Functional pAC50 = 4.8 4.8 -9 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 50235 None 31 Human Functional pAC50 = 4.8 4.8 -38 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 50235 None 31 Human Functional pAC50 = 4.8 4.8 -38 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 50235 None 31 Human Functional pAC50 = 4.8 4.8 -38 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 117027 None 19 Human Functional pAC50 = 4.8 4.8 -3 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 117027 None 19 Human Functional pAC50 = 4.8 4.8 -3 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 179242 None 69 Human Functional pAC50 = 4.8 4.8 -120 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 179242 None 69 Human Functional pAC50 = 4.8 4.8 -120 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 188375 None 19 Human Functional pAC50 = 4.8 4.8 -6 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 188375 None 19 Human Functional pAC50 = 4.8 4.8 -6 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 194829 None 40 Human Functional pAC50 = 4.8 4.8 -23 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 194829 None 40 Human Functional pAC50 = 4.8 4.8 -23 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 194829 None 40 Human Functional pAC50 = 4.8 4.8 -23 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 142422 None 66 Human Functional pAC50 = 5.8 5.8 -1 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 142422 None 66 Human Functional pAC50 = 5.8 5.8 -1 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 44861 None 29 Human Functional pAC50 = 5.8 5.8 -26 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 44861 None 29 Human Functional pAC50 = 5.8 5.8 -26 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206077 None 58 Human Functional pAC50 = 5.8 5.8 -36 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206077 None 58 Human Functional pAC50 = 5.8 5.8 -36 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 209982 None 33 Human Functional pAC50 = 5.8 5.8 -75 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
19861.0 209982 None 33 Human Functional pAC50 = 5.8 5.8 -75 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 209982 None 33 Human Functional pAC50 = 5.8 5.8 -75 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB00719 209982 None 33 Human Functional pAC50 = 5.8 5.8 -75 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
137 370 None 37 Human Functional pAC50 = 4.8 4.8 -7244 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 370 None 37 Human Functional pAC50 = 4.8 4.8 -7244 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
563 370 None 37 Human Functional pAC50 = 4.8 4.8 -7244 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 370 None 37 Human Functional pAC50 = 4.8 4.8 -7244 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 370 None 37 Human Functional pAC50 = 4.8 4.8 -7244 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 370 None 37 Human Functional pAC50 = 4.8 4.8 -7244 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 786 None 65 Human Functional pAC50 = 4.8 4.8 -8511 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2541.0 786 None 65 Human Functional pAC50 = 4.8 4.8 -8511 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
587 786 None 65 Human Functional pAC50 = 4.8 4.8 -8511 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 786 None 65 Human Functional pAC50 = 4.8 4.8 -8511 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 786 None 65 Human Functional pAC50 = 4.8 4.8 -8511 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 786 None 65 Human Functional pAC50 = 4.8 4.8 -8511 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 786 None 65 Human Functional pAC50 = 4.8 4.8 -8511 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 5720 None 27 Human Functional pAC50 = 4.8 4.8 -19 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4942.0 5720 None 27 Human Functional pAC50 = 4.8 4.8 -19 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 5720 None 27 Human Functional pAC50 = 4.8 4.8 -19 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB12278 5720 None 27 Human Functional pAC50 = 4.8 4.8 -19 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2546 None 55 Human Functional pAC50 = 4.8 4.8 -1548 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2546 None 55 Human Functional pAC50 = 4.8 4.8 -1548 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2546 None 55 Human Functional pAC50 = 4.8 4.8 -1548 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
65906.0 2546 None 55 Human Functional pAC50 = 4.8 4.8 -1548 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2546 None 55 Human Functional pAC50 = 4.8 4.8 -1548 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2546 None 55 Human Functional pAC50 = 4.8 4.8 -1548 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 31229 None 62 Human Functional pAC50 = 4.8 4.8 -38 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 31229 None 62 Human Functional pAC50 = 4.8 4.8 -38 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 59795 None 61 Human Functional pAC50 = 4.8 4.8 -8 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 59795 None 61 Human Functional pAC50 = 4.8 4.8 -8 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 8653 None 9 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 8653 None 9 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189192 None 17 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189192 None 17 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206377 None 46 Human Functional pAC50 = 4.8 4.8 -3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206377 None 46 Human Functional pAC50 = 4.8 4.8 -3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206707 None 55 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206707 None 55 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2762 None 13 Human Functional pAC50 = 6.8 6.8 -107 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2762 None 13 Human Functional pAC50 = 6.8 6.8 -107 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2762 None 13 Human Functional pAC50 = 6.8 6.8 -107 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2006 None 61 Human Functional pAC50 = 5.8 5.8 -1862 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2006 None 61 Human Functional pAC50 = 5.8 5.8 -1862 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
71360.0 2006 None 61 Human Functional pAC50 = 5.8 5.8 -1862 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2006 None 61 Human Functional pAC50 = 5.8 5.8 -1862 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2006 None 61 Human Functional pAC50 = 5.8 5.8 -1862 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2006 None 61 Human Functional pAC50 = 5.8 5.8 -1862 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -26 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -26 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -26 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5566.0 3860 None 43 Human Functional pAC50 = 5.7 5.7 -26 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -26 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -26 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3860 None 43 Human Functional pAC50 = 5.7 5.7 -26 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
37 778 None 41 Human Functional pAC50 = 6.7 6.7 -3 12
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
460 778 None 41 Human Functional pAC50 = 6.7 6.7 -3 12
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 778 None 41 Human Functional pAC50 = 6.7 6.7 -3 12
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
54746.0 778 None 41 Human Functional pAC50 = 6.7 6.7 -3 12
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 778 None 41 Human Functional pAC50 = 6.7 6.7 -3 12
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 778 None 41 Human Functional pAC50 = 6.7 6.7 -3 12
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 18873 None 78 Human Functional pAC50 = 4.7 4.7 -10 6
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 18873 None 78 Human Functional pAC50 = 4.7 4.7 -10 6
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 112646 None 60 Human Functional pAC50 = 4.7 4.7 -61 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 112646 None 60 Human Functional pAC50 = 4.7 4.7 -61 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 121354 None 36 Human Functional pAC50 = 4.7 4.7 -478 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 121354 None 36 Human Functional pAC50 = 4.7 4.7 -478 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9309 None 36 Human Functional pAC50 = 6.7 6.7 52 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9309 None 36 Human Functional pAC50 = 6.7 6.7 52 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78202 None 29 Human Functional pAC50 = 6.7 6.7 1 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
68867.0 78202 None 29 Human Functional pAC50 = 6.7 6.7 1 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78202 None 29 Human Functional pAC50 = 6.7 6.7 1 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB08810 78202 None 29 Human Functional pAC50 = 6.7 6.7 1 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 187026 None 38 Human Functional pAC50 = 4.7 4.7 -125 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 187026 None 38 Human Functional pAC50 = 4.7 4.7 -125 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 187026 None 38 Human Functional pAC50 = 4.7 4.7 -125 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 61580 None 50 Human Functional pAC50 = 5.7 5.7 1 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
60606.0 61580 None 50 Human Functional pAC50 = 5.7 5.7 1 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 61580 None 50 Human Functional pAC50 = 5.7 5.7 1 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB00758 61580 None 50 Human Functional pAC50 = 5.7 5.7 1 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 157623 None 57 Human Functional pAC50 = 5.7 5.7 1 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 157623 None 57 Human Functional pAC50 = 5.7 5.7 1 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2483 None 21 Human Functional pAC50 = 4.7 4.7 -33 17
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 2483 None 21 Human Functional pAC50 = 4.7 4.7 -33 17
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 2483 None 21 Human Functional pAC50 = 4.7 4.7 -33 17
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 2483 None 21 Human Functional pAC50 = 4.7 4.7 -33 17
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 56869 None 26 Human Functional pAC50 = 4.7 4.7 -58 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 56869 None 26 Human Functional pAC50 = 4.7 4.7 -58 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 56869 None 26 Human Functional pAC50 = 4.7 4.7 -58 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 97442 None 46 Human Functional pAC50 = 4.7 4.7 -2 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 97442 None 46 Human Functional pAC50 = 4.7 4.7 -2 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98949 None 48 Human Functional pAC50 = 4.7 4.7 -398 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98949 None 48 Human Functional pAC50 = 4.7 4.7 -398 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
198 313 None 72 Human Functional pAC50 = 5.7 5.7 -724 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 313 None 72 Human Functional pAC50 = 5.7 5.7 -724 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
82148.0 313 None 72 Human Functional pAC50 = 5.7 5.7 -724 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
99 313 None 72 Human Functional pAC50 = 5.7 5.7 -724 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 313 None 72 Human Functional pAC50 = 5.7 5.7 -724 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 313 None 72 Human Functional pAC50 = 5.7 5.7 -724 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 919 None 48 Human Functional pAC50 = 5.7 5.7 -134 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2726.0 919 None 48 Human Functional pAC50 = 5.7 5.7 -134 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
621 919 None 48 Human Functional pAC50 = 5.7 5.7 -134 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
83 919 None 48 Human Functional pAC50 = 5.7 5.7 -134 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 919 None 48 Human Functional pAC50 = 5.7 5.7 -134 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 919 None 48 Human Functional pAC50 = 5.7 5.7 -134 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 163278 None 34 Human Functional pAC50 = 4.7 4.7 -2454 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 163278 None 34 Human Functional pAC50 = 4.7 4.7 -2454 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 89164 None 10 Human Functional pAC50 = 4.7 4.7 -630 13
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 89164 None 10 Human Functional pAC50 = 4.7 4.7 -630 13
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 27039 None 53 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 27039 None 53 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 30706 None 19 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 30706 None 19 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 43468 None 43 Human Functional pAC50 = 4.7 4.7 -6 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 43468 None 43 Human Functional pAC50 = 4.7 4.7 -6 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1957 None 46 Human Functional pAC50 = 5.7 5.7 -4 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1957 None 46 Human Functional pAC50 = 5.7 5.7 -4 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3658.0 1957 None 46 Human Functional pAC50 = 5.7 5.7 -4 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1957 None 46 Human Functional pAC50 = 5.7 5.7 -4 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1957 None 46 Human Functional pAC50 = 5.7 5.7 -4 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1957 None 46 Human Functional pAC50 = 5.7 5.7 -4 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1957 None 46 Human Functional pAC50 = 5.7 5.7 -4 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 788 None 26 Human Functional pAC50 = 5.6 5.6 -35 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 788 None 26 Human Functional pAC50 = 5.6 5.6 -35 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 788 None 26 Human Functional pAC50 = 5.6 5.6 -35 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
644019.0 788 None 26 Human Functional pAC50 = 5.6 5.6 -35 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 788 None 26 Human Functional pAC50 = 5.6 5.6 -35 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 788 None 26 Human Functional pAC50 = 5.6 5.6 -35 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4143 None 47 Human Functional pAC50 = 6.6 6.6 -23 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4143 None 47 Human Functional pAC50 = 6.6 6.6 -23 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4143 None 47 Human Functional pAC50 = 6.6 6.6 -23 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
60854.0 4143 None 47 Human Functional pAC50 = 6.6 6.6 -23 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4143 None 47 Human Functional pAC50 = 6.6 6.6 -23 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4143 None 47 Human Functional pAC50 = 6.6 6.6 -23 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14476 None 26 Human Functional pAC50 = 6.6 6.6 -7 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14476 None 26 Human Functional pAC50 = 6.6 6.6 -7 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3132 None 63 Human Functional pAC50 = 5.6 5.6 -38 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3132 None 63 Human Functional pAC50 = 5.6 5.6 -38 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4850.0 3132 None 63 Human Functional pAC50 = 5.6 5.6 -38 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3132 None 63 Human Functional pAC50 = 5.6 5.6 -38 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3132 None 63 Human Functional pAC50 = 5.6 5.6 -38 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3132 None 63 Human Functional pAC50 = 5.6 5.6 -38 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 102826 None 36 Human Functional pAC50 = 5.6 5.6 -331 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 102826 None 36 Human Functional pAC50 = 5.6 5.6 -331 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 102826 None 36 Human Functional pAC50 = 5.6 5.6 -331 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14475 None 14 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14475 None 14 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 97442 None 46 Human Functional pAC50 = 4.6 4.6 -2 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 97442 None 46 Human Functional pAC50 = 4.6 4.6 -2 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 188732 None 57 Human Functional pAC50 = 4.6 4.6 -3548 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 188732 None 57 Human Functional pAC50 = 4.6 4.6 -3548 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 160344 None 54 Human Functional pAC50 = 4.6 4.6 -28 31
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 160344 None 54 Human Functional pAC50 = 4.6 4.6 -28 31
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 16656 None 34 Human Functional pAC50 = 4.6 4.6 -12 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 16656 None 34 Human Functional pAC50 = 4.6 4.6 -12 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 16656 None 34 Human Functional pAC50 = 4.6 4.6 -12 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 67012 None 31 Human Functional pAC50 = 4.6 4.6 -2 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 67012 None 31 Human Functional pAC50 = 4.6 4.6 -2 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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
3341.0 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 1628 None 36 Human Functional pAC50 = 6.6 6.6 -28 12
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 2509 None 14 Human Functional pAC50 = 7.6 7.6 -2 17
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 2509 None 14 Human Functional pAC50 = 7.6 7.6 -2 17
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 2509 None 14 Human Functional pAC50 = 7.6 7.6 -2 17
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
8226.0 2509 None 14 Human Functional pAC50 = 7.6 7.6 -2 17
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 2509 None 14 Human Functional pAC50 = 7.6 7.6 -2 17
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 2509 None 14 Human Functional pAC50 = 7.6 7.6 -2 17
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 729 None 28 Human Functional pAC50 = 4.6 4.6 -165 29
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
31101.0 729 None 28 Human Functional pAC50 = 4.6 4.6 -165 29
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
35 729 None 28 Human Functional pAC50 = 4.6 4.6 -165 29
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
403 729 None 28 Human Functional pAC50 = 4.6 4.6 -165 29
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 729 None 28 Human Functional pAC50 = 4.6 4.6 -165 29
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 729 None 28 Human Functional pAC50 = 4.6 4.6 -165 29
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 2483 None 21 Human Functional pAC50 = 4.6 4.6 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2483 None 21 Human Functional pAC50 = 4.6 4.6 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2483 None 21 Human Functional pAC50 = 4.6 4.6 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2483 None 21 Human Functional pAC50 = 4.6 4.6 -33 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14490 None 22 Human Functional pAC50 = 4.6 4.6 1 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14490 None 22 Human Functional pAC50 = 4.6 4.6 1 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 205585 None 33 Human Functional pAC50 = 4.6 4.6 -14 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 205585 None 33 Human Functional pAC50 = 4.6 4.6 -14 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 597 None 17 Human Functional pAC50 = 5.6 5.6 -208 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
1201549.0 597 None 17 Human Functional pAC50 = 5.6 5.6 -208 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
333 597 None 17 Human Functional pAC50 = 5.6 5.6 -208 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 597 None 17 Human Functional pAC50 = 5.6 5.6 -208 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 597 None 17 Human Functional pAC50 = 5.6 5.6 -208 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 597 None 17 Human Functional pAC50 = 5.6 5.6 -208 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 597 None 17 Human Functional pAC50 = 5.6 5.6 -208 26
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 43578 None 39 Human Functional pAC50 = 4.6 4.6 -2 3
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 43578 None 39 Human Functional pAC50 = 4.6 4.6 -2 3
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 1324 None 32 Human Functional pAC50 = 4.6 4.6 -8317 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1324 None 32 Human Functional pAC50 = 4.6 4.6 -8317 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1324 None 32 Human Functional pAC50 = 4.6 4.6 -8317 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
444031.0 1324 None 32 Human Functional pAC50 = 4.6 4.6 -8317 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1324 None 32 Human Functional pAC50 = 4.6 4.6 -8317 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1324 None 32 Human Functional pAC50 = 4.6 4.6 -8317 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1324 None 32 Human Functional pAC50 = 4.6 4.6 -8317 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3163 None 48 Human Functional pAC50 = 4.6 4.6 -22387 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3163 None 48 Human Functional pAC50 = 4.6 4.6 -22387 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4893.0 3163 None 48 Human Functional pAC50 = 4.6 4.6 -22387 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3163 None 48 Human Functional pAC50 = 4.6 4.6 -22387 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3163 None 48 Human Functional pAC50 = 4.6 4.6 -22387 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3163 None 48 Human Functional pAC50 = 4.6 4.6 -22387 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3163 None 48 Human Functional pAC50 = 4.6 4.6 -22387 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189074 None 0 Human Functional pAC50 = 4.6 4.6 -218 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 198347 None 44 Human Functional pAC50 = 4.6 4.6 -5 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 198347 None 44 Human Functional pAC50 = 4.6 4.6 -5 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 198347 None 44 Human Functional pAC50 = 4.6 4.6 -5 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 208438 None 30 Human Functional pAC50 = 4.6 4.6 -3 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 208438 None 30 Human Functional pAC50 = 4.6 4.6 -3 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4127 None 36 Human Functional pAC50 = 6.6 6.6 -16 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4127 None 36 Human Functional pAC50 = 6.6 6.6 -16 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4127 None 36 Human Functional pAC50 = 6.6 6.6 -16 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
8969.0 4127 None 36 Human Functional pAC50 = 6.6 6.6 -16 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4127 None 36 Human Functional pAC50 = 6.6 6.6 -16 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4127 None 36 Human Functional pAC50 = 6.6 6.6 -16 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 949 None 27 Human Functional pAC50 = 5.6 5.6 -263 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
26987.0 949 None 27 Human Functional pAC50 = 5.6 5.6 -263 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 949 None 27 Human Functional pAC50 = 5.6 5.6 -263 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
671 949 None 27 Human Functional pAC50 = 5.6 5.6 -263 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 949 None 27 Human Functional pAC50 = 5.6 5.6 -263 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 949 None 27 Human Functional pAC50 = 5.6 5.6 -263 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 17999 None 26 Human Functional pAC50 = 5.6 5.6 -2 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 17999 None 26 Human Functional pAC50 = 5.6 5.6 -2 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 178333 None 41 Human Functional pAC50 = 5.6 5.6 -4 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 178333 None 41 Human Functional pAC50 = 5.6 5.6 -4 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3805 None 44 Human Functional pAC50 = 5.6 5.6 -125 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3805 None 44 Human Functional pAC50 = 5.6 5.6 -125 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3805 None 44 Human Functional pAC50 = 5.6 5.6 -125 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3805 None 44 Human Functional pAC50 = 5.6 5.6 -125 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3805 None 44 Human Functional pAC50 = 5.6 5.6 -125 38
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2981 None 32 Human Functional pAC50 = 6.6 6.6 -457 24
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 2981 None 32 Human Functional pAC50 = 6.6 6.6 -457 24
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 2981 None 32 Human Functional pAC50 = 6.6 6.6 -457 24
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
4636.0 2981 None 32 Human Functional pAC50 = 6.6 6.6 -457 24
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 2981 None 32 Human Functional pAC50 = 6.6 6.6 -457 24
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 2981 None 32 Human Functional pAC50 = 6.6 6.6 -457 24
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 206863 None 31 Human Functional pAC50 = 4.6 4.6 -154 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2995.0 206863 None 31 Human Functional pAC50 = 4.6 4.6 -154 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206863 None 31 Human Functional pAC50 = 4.6 4.6 -154 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206863 None 31 Human Functional pAC50 = 4.6 4.6 -154 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB01151 206863 None 31 Human Functional pAC50 = 4.6 4.6 -154 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3134 None 58 Human Functional pAC50 = 7.6 7.6 -10 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3134 None 58 Human Functional pAC50 = 7.6 7.6 -10 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
27400.0 3134 None 58 Human Functional pAC50 = 7.6 7.6 -10 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3134 None 58 Human Functional pAC50 = 7.6 7.6 -10 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3134 None 58 Human Functional pAC50 = 7.6 7.6 -10 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3134 None 58 Human Functional pAC50 = 7.6 7.6 -10 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 203394 None 56 Human Functional pAC50 = 5.6 5.6 1 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 203394 None 56 Human Functional pAC50 = 5.6 5.6 1 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3853 None 34 Human Functional pAC50 = 6.6 6.6 -4 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3853 None 34 Human Functional pAC50 = 6.6 6.6 -4 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3853 None 34 Human Functional pAC50 = 6.6 6.6 -4 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5533.0 3853 None 34 Human Functional pAC50 = 6.6 6.6 -4 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3853 None 34 Human Functional pAC50 = 6.6 6.6 -4 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3853 None 34 Human Functional pAC50 = 6.6 6.6 -4 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3370 None 38 Human Functional pAC50 = 5.6 5.6 -512 17
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 3370 None 38 Human Functional pAC50 = 5.6 5.6 -512 17
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
5095.0 3370 None 38 Human Functional pAC50 = 5.6 5.6 -512 17
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 3370 None 38 Human Functional pAC50 = 5.6 5.6 -512 17
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 3370 None 38 Human Functional pAC50 = 5.6 5.6 -512 17
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 3370 None 38 Human Functional pAC50 = 5.6 5.6 -512 17
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 1420 None 13 Human Functional pAC50 = 5.6 5.6 -100 29
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
10531.0 1420 None 13 Human Functional pAC50 = 5.6 5.6 -100 29
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 1420 None 13 Human Functional pAC50 = 5.6 5.6 -100 29
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 1420 None 13 Human Functional pAC50 = 5.6 5.6 -100 29
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 1420 None 13 Human Functional pAC50 = 5.6 5.6 -100 29
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 1420 None 13 Human Functional pAC50 = 5.6 5.6 -100 29
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 3173 None 38 Human Functional pAC50 = 5.6 5.6 -35 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3173 None 38 Human Functional pAC50 = 5.6 5.6 -35 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4917.0 3173 None 38 Human Functional pAC50 = 5.6 5.6 -35 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3173 None 38 Human Functional pAC50 = 5.6 5.6 -35 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3173 None 38 Human Functional pAC50 = 5.6 5.6 -35 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3173 None 38 Human Functional pAC50 = 5.6 5.6 -35 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 209699 None 30 Human Functional pAC50 = 5.6 5.6 -4 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 209699 None 30 Human Functional pAC50 = 5.6 5.6 -4 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 5162 None 41 Human Functional pAC50 = 4.6 4.6 -7 2
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 5162 None 41 Human Functional pAC50 = 4.6 4.6 -7 2
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 5162 None 41 Human Functional pAC50 = 4.6 4.6 -7 2
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 4301 None 35 Human Functional pAC50 = 4.6 4.6 -12 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4301 None 35 Human Functional pAC50 = 4.6 4.6 -12 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4301 None 35 Human Functional pAC50 = 4.6 4.6 -12 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 112647 None 47 Human Functional pAC50 = 4.6 4.6 -3 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 112647 None 47 Human Functional pAC50 = 4.6 4.6 -3 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 178724 None 43 Human Functional pAC50 = 5.5 5.5 -6 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 178724 None 43 Human Functional pAC50 = 5.5 5.5 -6 19
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14505 None 4 Human Functional pAC50 = 4.5 4.5 -177 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
6127.0 14505 None 4 Human Functional pAC50 = 4.5 4.5 -177 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14505 None 4 Human Functional pAC50 = 4.5 4.5 -177 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB13720 14505 None 4 Human Functional pAC50 = 4.5 4.5 -177 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 30492 None 42 Human Functional pAC50 = 4.5 4.5 -2 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 30492 None 42 Human Functional pAC50 = 4.5 4.5 -2 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98126 None 43 Human Functional pAC50 = 4.5 4.5 -9 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98126 None 43 Human Functional pAC50 = 4.5 4.5 -9 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 208386 None 26 Human Functional pAC50 = 4.5 4.5 -46 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5467.0 208386 None 26 Human Functional pAC50 = 4.5 4.5 -46 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 208386 None 26 Human Functional pAC50 = 4.5 4.5 -46 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB13025 208386 None 26 Human Functional pAC50 = 4.5 4.5 -46 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 209393 None 28 Human Functional pAC50 = 4.5 4.5 -138 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 209393 None 28 Human Functional pAC50 = 4.5 4.5 -138 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
37 778 None 41 Human Functional pAC50 = 8.5 8.5 -3 12
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
460 778 None 41 Human Functional pAC50 = 8.5 8.5 -3 12
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 778 None 41 Human Functional pAC50 = 8.5 8.5 -3 12
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
54746.0 778 None 41 Human Functional pAC50 = 8.5 8.5 -3 12
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 778 None 41 Human Functional pAC50 = 8.5 8.5 -3 12
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 778 None 41 Human Functional pAC50 = 8.5 8.5 -3 12
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 2532 None 33 Human Functional pAC50 = 7.5 7.5 -5 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2532 None 33 Human Functional pAC50 = 7.5 7.5 -5 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2532 None 33 Human Functional pAC50 = 7.5 7.5 -5 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4184.0 2532 None 33 Human Functional pAC50 = 7.5 7.5 -5 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2532 None 33 Human Functional pAC50 = 7.5 7.5 -5 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2532 None 33 Human Functional pAC50 = 7.5 7.5 -5 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 89164 None 10 Human Functional pAC50 = 5.5 5.5 -630 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 89164 None 10 Human Functional pAC50 = 5.5 5.5 -630 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
242 470 None 70 Human Functional pAC50 = 6.5 6.5 -33 33
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
34 470 None 70 Human Functional pAC50 = 6.5 6.5 -33 33
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 470 None 70 Human Functional pAC50 = 6.5 6.5 -33 33
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
60795.0 470 None 70 Human Functional pAC50 = 6.5 6.5 -33 33
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 470 None 70 Human Functional pAC50 = 6.5 6.5 -33 33
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 470 None 70 Human Functional pAC50 = 6.5 6.5 -33 33
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 84687 None 24 Human Functional pAC50 = 5.5 5.5 -33 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 84687 None 24 Human Functional pAC50 = 5.5 5.5 -33 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 35070 None 5 Human Functional pAC50 = 5.5 5.5 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 35070 None 5 Human Functional pAC50 = 5.5 5.5 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 35070 None 5 Human Functional pAC50 = 5.5 5.5 -2 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207084 None 54 Human Functional pAC50 = 5.5 5.5 -194 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4066.0 207084 None 54 Human Functional pAC50 = 5.5 5.5 -194 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207084 None 54 Human Functional pAC50 = 5.5 5.5 -194 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB01071 207084 None 54 Human Functional pAC50 = 5.5 5.5 -194 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 599 None 30 Human Functional pAC50 = 6.5 6.5 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
331 599 None 30 Human Functional pAC50 = 6.5 6.5 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 599 None 30 Human Functional pAC50 = 6.5 6.5 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 599 None 30 Human Functional pAC50 = 6.5 6.5 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 599 None 30 Human Functional pAC50 = 6.5 6.5 3 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 10802 None 64 Human Functional pAC50 = 5.5 5.5 -10 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 10802 None 64 Human Functional pAC50 = 5.5 5.5 -10 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206491 None 57 Human Functional pAC50 = 4.5 4.5 -11220 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206491 None 57 Human Functional pAC50 = 4.5 4.5 -11220 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3773 None 26 Human Functional pAC50 = 6.5 6.5 -28 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3773 None 26 Human Functional pAC50 = 6.5 6.5 -28 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3773 None 26 Human Functional pAC50 = 6.5 6.5 -28 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2066 None 66 Human Functional pAC50 = 4.5 4.5 -38904 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2066 None 66 Human Functional pAC50 = 4.5 4.5 -38904 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3749.0 2066 None 66 Human Functional pAC50 = 4.5 4.5 -38904 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2066 None 66 Human Functional pAC50 = 4.5 4.5 -38904 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2066 None 66 Human Functional pAC50 = 4.5 4.5 -38904 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2066 None 66 Human Functional pAC50 = 4.5 4.5 -38904 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2066 None 66 Human Functional pAC50 = 4.5 4.5 -38904 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1889 None 43 Human Functional pAC50 = 6.5 6.5 -79 12
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 1889 None 43 Human Functional pAC50 = 6.5 6.5 -79 12
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
3519.0 1889 None 43 Human Functional pAC50 = 6.5 6.5 -79 12
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 1889 None 43 Human Functional pAC50 = 6.5 6.5 -79 12
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 1889 None 43 Human Functional pAC50 = 6.5 6.5 -79 12
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 1889 None 43 Human Functional pAC50 = 6.5 6.5 -79 12
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 2027 None 69 Human Functional pAC50 = 4.4 4.4 -93 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2027 None 69 Human Functional pAC50 = 4.4 4.4 -93 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2027 None 69 Human Functional pAC50 = 4.4 4.4 -93 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2027 None 69 Human Functional pAC50 = 4.4 4.4 -93 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2027 None 69 Human Functional pAC50 = 4.4 4.4 -93 7
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14417 None 47 Human Functional pAC50 = 4.4 4.4 -15 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14417 None 47 Human Functional pAC50 = 4.4 4.4 -15 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 41735 None 12 Human Functional pAC50 = 5.4 5.4 -190 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5284550.0 41735 None 12 Human Functional pAC50 = 5.4 5.4 -190 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
CHEMBL108947 41735 None 12 Human Functional pAC50 = 5.4 5.4 -190 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 41735 None 12 Human Functional pAC50 = 5.4 5.4 -190 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB09167 41735 None 12 Human Functional pAC50 = 5.4 5.4 -190 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
240 944 None 25 Human Functional pAC50 = 5.4 5.4 -79 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 944 None 25 Human Functional pAC50 = 5.4 5.4 -79 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 944 None 25 Human Functional pAC50 = 5.4 5.4 -79 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
660 944 None 25 Human Functional pAC50 = 5.4 5.4 -79 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 944 None 25 Human Functional pAC50 = 5.4 5.4 -79 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 944 None 25 Human Functional pAC50 = 5.4 5.4 -79 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 944 None 25 Human Functional pAC50 = 5.4 5.4 -79 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 84404 None 3 Human Functional pAC50 = 5.4 5.4 -389 11
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
55645.0 84404 None 3 Human Functional pAC50 = 5.4 5.4 -389 11
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 84404 None 3 Human Functional pAC50 = 5.4 5.4 -389 11
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 122423 None 61 Human Functional pAC50 = 4.4 4.4 -5 5
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 122423 None 61 Human Functional pAC50 = 4.4 4.4 -5 5
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 5260 None 48 Human Functional pAC50 = 5.4 5.4 -1 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 5260 None 48 Human Functional pAC50 = 5.4 5.4 -1 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206037 None 20 Human Functional pAC50 = 5.4 5.4 -426 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 206037 None 20 Human Functional pAC50 = 5.4 5.4 -426 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2514 None 19 Human Functional pAC50 = 8.4 8.4 2 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2514 None 19 Human Functional pAC50 = 8.4 8.4 2 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2514 None 19 Human Functional pAC50 = 8.4 8.4 2 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
9681.0 2514 None 19 Human Functional pAC50 = 8.4 8.4 2 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2514 None 19 Human Functional pAC50 = 8.4 8.4 2 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2514 None 19 Human Functional pAC50 = 8.4 8.4 2 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 120581 None 50 Human Functional pAC50 = 5.4 5.4 2 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 120581 None 50 Human Functional pAC50 = 5.4 5.4 2 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3256 None 51 Human Functional pAC50 = 5.4 5.4 -11 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3256 None 51 Human Functional pAC50 = 5.4 5.4 -11 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3256 None 51 Human Functional pAC50 = 5.4 5.4 -11 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5002.0 3256 None 51 Human Functional pAC50 = 5.4 5.4 -11 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3256 None 51 Human Functional pAC50 = 5.4 5.4 -11 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3256 None 51 Human Functional pAC50 = 5.4 5.4 -11 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -128 17
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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -128 17
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
59227.0 3372 None 50 Human Functional pAC50 = 6.4 6.4 -128 17
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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -128 17
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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -128 17
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 3372 None 50 Human Functional pAC50 = 6.4 6.4 -128 17
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 2518 None 51 Human Functional pAC50 = 5.4 5.4 -45 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2518 None 51 Human Functional pAC50 = 5.4 5.4 -45 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2518 None 51 Human Functional pAC50 = 5.4 5.4 -45 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4168.0 2518 None 51 Human Functional pAC50 = 5.4 5.4 -45 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2518 None 51 Human Functional pAC50 = 5.4 5.4 -45 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2518 None 51 Human Functional pAC50 = 5.4 5.4 -45 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3779 None 53 Human Functional pAC50 = 5.4 5.4 -15 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3779 None 53 Human Functional pAC50 = 5.4 5.4 -15 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3779 None 53 Human Functional pAC50 = 5.4 5.4 -15 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3779 None 53 Human Functional pAC50 = 5.4 5.4 -15 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3779 None 53 Human Functional pAC50 = 5.4 5.4 -15 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 56328 None 57 Human Functional pAC50 = 5.4 5.4 -3 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 56328 None 57 Human Functional pAC50 = 5.4 5.4 -3 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9159 None 27 Human Functional pAC50 = 5.4 5.4 -117 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9159 None 27 Human Functional pAC50 = 5.4 5.4 -117 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9838 None 41 Human Functional pAC50 = 4.4 4.4 -288 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9838 None 41 Human Functional pAC50 = 4.4 4.4 -288 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 175250 None 68 Human Functional pAC50 = 5.4 5.4 3 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 175250 None 68 Human Functional pAC50 = 5.4 5.4 3 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3331 None 72 Human Functional pAC50 = 6.4 6.4 -91 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3331 None 72 Human Functional pAC50 = 6.4 6.4 -91 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5073.0 3331 None 72 Human Functional pAC50 = 6.4 6.4 -91 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3331 None 72 Human Functional pAC50 = 6.4 6.4 -91 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3331 None 72 Human Functional pAC50 = 6.4 6.4 -91 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3331 None 72 Human Functional pAC50 = 6.4 6.4 -91 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 7074 None 25 Human Functional pAC50 = 5.4 5.4 -1023 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
17676.0 7074 None 25 Human Functional pAC50 = 5.4 5.4 -1023 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 7074 None 25 Human Functional pAC50 = 5.4 5.4 -1023 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 7074 None 25 Human Functional pAC50 = 5.4 5.4 -1023 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB01063 7074 None 25 Human Functional pAC50 = 5.4 5.4 -1023 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3125 None 49 Human Functional pAC50 = 4.4 4.4 -371 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
16362.0 3125 None 49 Human Functional pAC50 = 4.4 4.4 -371 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3125 None 49 Human Functional pAC50 = 4.4 4.4 -371 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3125 None 49 Human Functional pAC50 = 4.4 4.4 -371 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3125 None 49 Human Functional pAC50 = 4.4 4.4 -371 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3125 None 49 Human Functional pAC50 = 4.4 4.4 -371 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189720 None 60 Human Functional pAC50 = 5.4 5.4 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189720 None 60 Human Functional pAC50 = 5.4 5.4 - 1
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 958 None 57 Human Functional pAC50 = 7.3 7.3 -8 43
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
135398737.0 958 None 57 Human Functional pAC50 = 7.3 7.3 -8 43
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
38 958 None 57 Human Functional pAC50 = 7.3 7.3 -8 43
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
722 958 None 57 Human Functional pAC50 = 7.3 7.3 -8 43
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 958 None 57 Human Functional pAC50 = 7.3 7.3 -8 43
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 958 None 57 Human Functional pAC50 = 7.3 7.3 -8 43
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1664 None 37 Human Functional pAC50 = 5.3 5.3 -107 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1664 None 37 Human Functional pAC50 = 5.3 5.3 -107 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3396.0 1664 None 37 Human Functional pAC50 = 5.3 5.3 -107 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1664 None 37 Human Functional pAC50 = 5.3 5.3 -107 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1664 None 37 Human Functional pAC50 = 5.3 5.3 -107 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1664 None 37 Human Functional pAC50 = 5.3 5.3 -107 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
228 445 None 20 Human Functional pAC50 = 5.3 5.3 -575 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
33 445 None 20 Human Functional pAC50 = 5.3 5.3 -575 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 445 None 20 Human Functional pAC50 = 5.3 5.3 -575 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
6005.0 445 None 20 Human Functional pAC50 = 5.3 5.3 -575 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 445 None 20 Human Functional pAC50 = 5.3 5.3 -575 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 445 None 20 Human Functional pAC50 = 5.3 5.3 -575 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 51685 None 37 Human Functional pAC50 = 5.3 5.3 -363 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 51685 None 37 Human Functional pAC50 = 5.3 5.3 -363 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 60100 None 66 Human Functional pAC50 = 6.3 6.3 1 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 60100 None 66 Human Functional pAC50 = 6.3 6.3 1 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3806 None 35 Human Functional pAC50 = 5.3 5.3 -758 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3806 None 35 Human Functional pAC50 = 5.3 5.3 -758 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3806 None 35 Human Functional pAC50 = 5.3 5.3 -758 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
941651.0 3806 None 35 Human Functional pAC50 = 5.3 5.3 -758 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3806 None 35 Human Functional pAC50 = 5.3 5.3 -758 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3806 None 35 Human Functional pAC50 = 5.3 5.3 -758 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 154946 None 18 Human Functional pAC50 = 6.3 6.3 3 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 154946 None 18 Human Functional pAC50 = 6.3 6.3 3 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2013 None 42 Human Functional pAC50 = 5.3 5.3 -1621 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2013 None 42 Human Functional pAC50 = 5.3 5.3 -1621 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2013 None 42 Human Functional pAC50 = 5.3 5.3 -1621 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2013 None 42 Human Functional pAC50 = 5.3 5.3 -1621 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2013 None 42 Human Functional pAC50 = 5.3 5.3 -1621 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2303 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4946 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
564 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
63 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
91536 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL27 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL452861 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
DB00571 3187 None 44 Human Functional pAC50 = 5.3 5.3 -389 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
5329102 194838 None 50 Human Functional pAC50 = 5.3 5.3 -8 37
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 194838 None 50 Human Functional pAC50 = 5.3 5.3 -8 37
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3653 None 40 Human Functional pAC50 = 5.3 5.3 -30902 23
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 3653 None 40 Human Functional pAC50 = 5.3 5.3 -30902 23
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 3653 None 40 Human Functional pAC50 = 5.3 5.3 -30902 23
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 3653 None 40 Human Functional pAC50 = 5.3 5.3 -30902 23
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 3653 None 40 Human Functional pAC50 = 5.3 5.3 -30902 23
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 78218 None 21 Human Functional pAC50 = 5.3 5.3 3 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78218 None 21 Human Functional pAC50 = 5.3 5.3 3 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 803 None 59 Human Functional pAC50 = 6.3 6.3 -64 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2585.0 803 None 59 Human Functional pAC50 = 6.3 6.3 -64 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
522 803 None 59 Human Functional pAC50 = 6.3 6.3 -64 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
551 803 None 59 Human Functional pAC50 = 6.3 6.3 -64 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 803 None 59 Human Functional pAC50 = 6.3 6.3 -64 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 803 None 59 Human Functional pAC50 = 6.3 6.3 -64 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 729 None 28 Human Functional pAC50 = 6.3 6.3 -165 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
31101.0 729 None 28 Human Functional pAC50 = 6.3 6.3 -165 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
35 729 None 28 Human Functional pAC50 = 6.3 6.3 -165 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
403 729 None 28 Human Functional pAC50 = 6.3 6.3 -165 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 729 None 28 Human Functional pAC50 = 6.3 6.3 -165 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 729 None 28 Human Functional pAC50 = 6.3 6.3 -165 29
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2914 None 65 Human Functional pAC50 = 7.3 7.3 -4 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
135398745.0 2914 None 65 Human Functional pAC50 = 7.3 7.3 -4 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2914 None 65 Human Functional pAC50 = 7.3 7.3 -4 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2914 None 65 Human Functional pAC50 = 7.3 7.3 -4 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2914 None 65 Human Functional pAC50 = 7.3 7.3 -4 33
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 559 None 45 Human Functional pAC50 = 5.3 5.3 -223 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2267.0 559 None 45 Human Functional pAC50 = 5.3 5.3 -223 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
271 559 None 45 Human Functional pAC50 = 5.3 5.3 -223 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 559 None 45 Human Functional pAC50 = 5.3 5.3 -223 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 559 None 45 Human Functional pAC50 = 5.3 5.3 -223 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 559 None 45 Human Functional pAC50 = 5.3 5.3 -223 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1414 None 26 Human Functional pAC50 = 5.3 5.3 -1096 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3042.0 1414 None 26 Human Functional pAC50 = 5.3 5.3 -1096 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1414 None 26 Human Functional pAC50 = 5.3 5.3 -1096 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1414 None 26 Human Functional pAC50 = 5.3 5.3 -1096 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1414 None 26 Human Functional pAC50 = 5.3 5.3 -1096 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1414 None 26 Human Functional pAC50 = 5.3 5.3 -1096 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98899 None 29 Human Functional pAC50 = 5.3 5.3 -9 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98899 None 29 Human Functional pAC50 = 5.3 5.3 -9 3
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 954 None 43 Human Functional pAC50 = 5.3 5.3 -831 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 954 None 43 Human Functional pAC50 = 5.3 5.3 -831 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2801.0 954 None 43 Human Functional pAC50 = 5.3 5.3 -831 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
701 954 None 43 Human Functional pAC50 = 5.3 5.3 -831 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 954 None 43 Human Functional pAC50 = 5.3 5.3 -831 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 954 None 43 Human Functional pAC50 = 5.3 5.3 -831 36
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3182 None 26 Human Functional pAC50 = 5.2 5.2 -89 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3182 None 26 Human Functional pAC50 = 5.2 5.2 -89 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3182 None 26 Human Functional pAC50 = 5.2 5.2 -89 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3182 None 26 Human Functional pAC50 = 5.2 5.2 -89 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3182 None 26 Human Functional pAC50 = 5.2 5.2 -89 34
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 162321 None 58 Human Functional pAC50 = 5.2 5.2 -1 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 162321 None 58 Human Functional pAC50 = 5.2 5.2 -1 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1633 None 50 Human Functional pAC50 = 5.2 5.2 -109 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1633 None 50 Human Functional pAC50 = 5.2 5.2 -109 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3348.0 1633 None 50 Human Functional pAC50 = 5.2 5.2 -109 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1633 None 50 Human Functional pAC50 = 5.2 5.2 -109 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1633 None 50 Human Functional pAC50 = 5.2 5.2 -109 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1633 None 50 Human Functional pAC50 = 5.2 5.2 -109 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1633 None 50 Human Functional pAC50 = 5.2 5.2 -109 5
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3780 None 25 Human Functional pAC50 = 6.2 6.2 -186 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3780 None 25 Human Functional pAC50 = 6.2 6.2 -186 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3780 None 25 Human Functional pAC50 = 6.2 6.2 -186 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3780 None 25 Human Functional pAC50 = 6.2 6.2 -186 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3780 None 25 Human Functional pAC50 = 6.2 6.2 -186 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78250 None 62 Human Functional pAC50 = 5.2 5.2 -4 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78250 None 62 Human Functional pAC50 = 5.2 5.2 -4 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 100668 None 35 Human Functional pAC50 = 5.2 5.2 -6 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 100668 None 35 Human Functional pAC50 = 5.2 5.2 -6 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3590 None 59 Human Functional pAC50 = 6.2 6.2 -20 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3590 None 59 Human Functional pAC50 = 6.2 6.2 -20 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3590 None 59 Human Functional pAC50 = 6.2 6.2 -20 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3590 None 59 Human Functional pAC50 = 6.2 6.2 -20 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3590 None 59 Human Functional pAC50 = 6.2 6.2 -20 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3095 None 24 Human Functional pAC50 = 5.2 5.2 -120 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3095 None 24 Human Functional pAC50 = 5.2 5.2 -120 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4768.0 3095 None 24 Human Functional pAC50 = 5.2 5.2 -120 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3095 None 24 Human Functional pAC50 = 5.2 5.2 -120 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3095 None 24 Human Functional pAC50 = 5.2 5.2 -120 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3095 None 24 Human Functional pAC50 = 5.2 5.2 -120 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 964 None 47 Human Functional pAC50 = 5.2 5.2 -6 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 964 None 47 Human Functional pAC50 = 5.2 5.2 -6 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
726 964 None 47 Human Functional pAC50 = 5.2 5.2 -6 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 964 None 47 Human Functional pAC50 = 5.2 5.2 -6 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 964 None 47 Human Functional pAC50 = 5.2 5.2 -6 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 505 None 55 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
249 505 None 55 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 505 None 55 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 505 None 55 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 505 None 55 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1470 None 44 Human Functional pAC50 = 5.2 5.2 -1318 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3157.0 1470 None 44 Human Functional pAC50 = 5.2 5.2 -1318 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1470 None 44 Human Functional pAC50 = 5.2 5.2 -1318 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1470 None 44 Human Functional pAC50 = 5.2 5.2 -1318 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1470 None 44 Human Functional pAC50 = 5.2 5.2 -1318 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1470 None 44 Human Functional pAC50 = 5.2 5.2 -1318 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 216518 None 10 Human Functional pAC50 = 7.2 7.2 -20 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 33583 None 70 Human Functional pAC50 = 5.2 5.2 -1 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 33583 None 70 Human Functional pAC50 = 5.2 5.2 -1 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
CHEMBL5416410 33583 None 70 Human Functional pAC50 = 5.2 5.2 -1 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3776 None 69 Human Functional pAC50 = 5.2 5.2 -3548 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3776 None 69 Human Functional pAC50 = 5.2 5.2 -3548 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3776 None 69 Human Functional pAC50 = 5.2 5.2 -3548 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
65999.0 3776 None 69 Human Functional pAC50 = 5.2 5.2 -3548 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3776 None 69 Human Functional pAC50 = 5.2 5.2 -3548 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3776 None 69 Human Functional pAC50 = 5.2 5.2 -3548 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4153 None 44 Human Functional pAC50 = 7.2 7.2 -6 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4153 None 44 Human Functional pAC50 = 7.2 7.2 -6 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4153 None 44 Human Functional pAC50 = 7.2 7.2 -6 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4153 None 44 Human Functional pAC50 = 7.2 7.2 -6 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4153 None 44 Human Functional pAC50 = 7.2 7.2 -6 22
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3749 None 48 Human Functional pAC50 = 5.2 5.2 -14125 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
129211.0 3749 None 48 Human Functional pAC50 = 5.2 5.2 -14125 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3749 None 48 Human Functional pAC50 = 5.2 5.2 -14125 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3749 None 48 Human Functional pAC50 = 5.2 5.2 -14125 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3749 None 48 Human Functional pAC50 = 5.2 5.2 -14125 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3749 None 48 Human Functional pAC50 = 5.2 5.2 -14125 14
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 596 None 33 Human Functional pAC50 = 5.2 5.2 -1258 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
16363.0 596 None 33 Human Functional pAC50 = 5.2 5.2 -1258 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
312 596 None 33 Human Functional pAC50 = 5.2 5.2 -1258 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 596 None 33 Human Functional pAC50 = 5.2 5.2 -1258 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 596 None 33 Human Functional pAC50 = 5.2 5.2 -1258 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 596 None 33 Human Functional pAC50 = 5.2 5.2 -1258 21
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207010 None 50 Human Functional pAC50 = 5.2 5.2 -1 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207010 None 50 Human Functional pAC50 = 5.2 5.2 -1 6
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2923 None 40 Human Functional pAC50 = 5.2 5.2 -50118 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
11504295.0 2923 None 40 Human Functional pAC50 = 5.2 5.2 -50118 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2923 None 40 Human Functional pAC50 = 5.2 5.2 -50118 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2923 None 40 Human Functional pAC50 = 5.2 5.2 -50118 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2923 None 40 Human Functional pAC50 = 5.2 5.2 -50118 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2923 None 40 Human Functional pAC50 = 5.2 5.2 -50118 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 32008 None 48 Human Functional pAC50 = 6.2 6.2 -199 8
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 32008 None 48 Human Functional pAC50 = 6.2 6.2 -199 8
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 32008 None 48 Human Functional pAC50 = 6.2 6.2 -199 8
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 1911 None 63 Human Functional pAC50 = 5.2 5.2 -851 39
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1911 None 63 Human Functional pAC50 = 5.2 5.2 -851 39
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3559.0 1911 None 63 Human Functional pAC50 = 5.2 5.2 -851 39
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1911 None 63 Human Functional pAC50 = 5.2 5.2 -851 39
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1911 None 63 Human Functional pAC50 = 5.2 5.2 -851 39
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1911 None 63 Human Functional pAC50 = 5.2 5.2 -851 39
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 197264 None 50 Human Functional pAC50 = 6.2 6.2 -5 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 197264 None 50 Human Functional pAC50 = 6.2 6.2 -5 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 197264 None 50 Human Functional pAC50 = 6.2 6.2 -5 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2540 None 64 Human Functional pAC50 = 5.2 5.2 -1047 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2540 None 64 Human Functional pAC50 = 5.2 5.2 -1047 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4205.0 2540 None 64 Human Functional pAC50 = 5.2 5.2 -1047 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2540 None 64 Human Functional pAC50 = 5.2 5.2 -1047 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2540 None 64 Human Functional pAC50 = 5.2 5.2 -1047 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2540 None 64 Human Functional pAC50 = 5.2 5.2 -1047 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 69401 None 70 Human Functional pAC50 = 5.2 5.2 -42 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 69401 None 70 Human Functional pAC50 = 5.2 5.2 -42 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9950 None 29 Human Functional pAC50 = 5.2 5.2 -41 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 9950 None 29 Human Functional pAC50 = 5.2 5.2 -41 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
179 400 None 72 Human Functional pAC50 = 6.2 6.2 -102 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 400 None 72 Human Functional pAC50 = 6.2 6.2 -102 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2159.0 400 None 72 Human Functional pAC50 = 6.2 6.2 -102 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
963 400 None 72 Human Functional pAC50 = 6.2 6.2 -102 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 400 None 72 Human Functional pAC50 = 6.2 6.2 -102 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 400 None 72 Human Functional pAC50 = 6.2 6.2 -102 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2385 None 44 Human Functional pAC50 = 7.2 7.2 -4 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
213046.0 2385 None 44 Human Functional pAC50 = 7.2 7.2 -4 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2385 None 44 Human Functional pAC50 = 7.2 7.2 -4 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2385 None 44 Human Functional pAC50 = 7.2 7.2 -4 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2385 None 44 Human Functional pAC50 = 7.2 7.2 -4 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2385 None 44 Human Functional pAC50 = 7.2 7.2 -4 17
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2866 None 32 Human Functional pAC50 = 6.1 6.1 -165 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2866 None 32 Human Functional pAC50 = 6.1 6.1 -165 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2866 None 32 Human Functional pAC50 = 6.1 6.1 -165 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4543.0 2866 None 32 Human Functional pAC50 = 6.1 6.1 -165 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2866 None 32 Human Functional pAC50 = 6.1 6.1 -165 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2866 None 32 Human Functional pAC50 = 6.1 6.1 -165 32
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 99377 None 50 Human Functional pAC50 = 5.1 5.1 -331 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2448.0 99377 None 50 Human Functional pAC50 = 5.1 5.1 -331 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 99377 None 50 Human Functional pAC50 = 5.1 5.1 -331 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB12401 99377 None 50 Human Functional pAC50 = 5.1 5.1 -331 15
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2590 None 33 Human Functional pAC50 = 6.1 6.1 -8 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2590 None 33 Human Functional pAC50 = 6.1 6.1 -8 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2590 None 33 Human Functional pAC50 = 6.1 6.1 -8 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
23897.0 2590 None 33 Human Functional pAC50 = 6.1 6.1 -8 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2590 None 33 Human Functional pAC50 = 6.1 6.1 -8 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2590 None 33 Human Functional pAC50 = 6.1 6.1 -8 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 745 None 38 Human Functional pAC50 = 5.1 5.1 -104 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2477.0 745 None 38 Human Functional pAC50 = 5.1 5.1 -104 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
36 745 None 38 Human Functional pAC50 = 5.1 5.1 -104 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
437 745 None 38 Human Functional pAC50 = 5.1 5.1 -104 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 745 None 38 Human Functional pAC50 = 5.1 5.1 -104 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 745 None 38 Human Functional pAC50 = 5.1 5.1 -104 20
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14501 None 15 Human Functional pAC50 = 5.1 5.1 1 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5906.0 14501 None 15 Human Functional pAC50 = 5.1 5.1 1 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14501 None 15 Human Functional pAC50 = 5.1 5.1 1 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB00610 14501 None 15 Human Functional pAC50 = 5.1 5.1 1 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 84720 None 41 Human Functional pAC50 = 5.1 5.1 -1 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 84720 None 41 Human Functional pAC50 = 5.1 5.1 -1 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207985 None 33 Human Functional pAC50 = 5.1 5.1 -14 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207985 None 33 Human Functional pAC50 = 5.1 5.1 -14 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 207985 None 33 Human Functional pAC50 = 5.1 5.1 -14 30
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 96601 None 25 Human Functional pAC50 = 6.1 6.1 1 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 96601 None 25 Human Functional pAC50 = 6.1 6.1 1 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3057 None 57 Human Functional pAC50 = 6.1 6.1 -338 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3057 None 57 Human Functional pAC50 = 6.1 6.1 -338 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3057 None 57 Human Functional pAC50 = 6.1 6.1 -338 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4748.0 3057 None 57 Human Functional pAC50 = 6.1 6.1 -338 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3057 None 57 Human Functional pAC50 = 6.1 6.1 -338 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3057 None 57 Human Functional pAC50 = 6.1 6.1 -338 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4402 None 68 Human Functional pAC50 = 5.1 5.1 -1122 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 4402 None 68 Human Functional pAC50 = 5.1 5.1 -1122 28
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1662 None 37 Human Functional pAC50 = 6.1 6.1 -60 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1662 None 37 Human Functional pAC50 = 6.1 6.1 -60 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1662 None 37 Human Functional pAC50 = 6.1 6.1 -60 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3372.0 1662 None 37 Human Functional pAC50 = 6.1 6.1 -60 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1662 None 37 Human Functional pAC50 = 6.1 6.1 -60 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 1662 None 37 Human Functional pAC50 = 6.1 6.1 -60 35
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 115628 None 61 Human Functional pAC50 = 6.1 6.1 -2 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 115628 None 61 Human Functional pAC50 = 6.1 6.1 -2 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 34231 None 58 Human Functional pAC50 = 6.1 6.1 -3 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4418.0 34231 None 58 Human Functional pAC50 = 6.1 6.1 -3 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 34231 None 58 Human Functional pAC50 = 6.1 6.1 -3 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB12092 34231 None 58 Human Functional pAC50 = 6.1 6.1 -3 18
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98061 None 34 Human Functional pAC50 = 5.1 5.1 -8 9
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 98061 None 34 Human Functional pAC50 = 5.1 5.1 -8 9
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 198259 None 39 Human Functional pAC50 = 5.1 5.1 3 2
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 198259 None 39 Human Functional pAC50 = 5.1 5.1 3 2
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189330 None 32 Human Functional pAC50 = 6.1 6.1 9 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189330 None 32 Human Functional pAC50 = 6.1 6.1 9 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 189330 None 32 Human Functional pAC50 = 6.1 6.1 9 10
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 11069 None 60 Human Functional pAC50 = 5.1 5.1 2 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 11069 None 60 Human Functional pAC50 = 5.1 5.1 2 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
189562 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
189562.0 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
71301.0 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
9844194 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
9844194.0 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
CHEMBL2365658 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
CHEMBL3526436 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2757 None 41 Human Functional pAC50 = 5.1 5.1 -2884 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14498 None 13 Human Functional pAC50 = 5.1 5.1 -239 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14498 None 13 Human Functional pAC50 = 5.1 5.1 -239 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14498 None 13 Human Functional pAC50 = 5.1 5.1 -239 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14498 None 13 Human Functional pAC50 = 5.1 5.1 -239 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 167007 None 49 Human Functional pAC50 = 5.1 5.1 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 167007 None 49 Human Functional pAC50 = 5.1 5.1 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 167007 None 49 Human Functional pAC50 = 5.1 5.1 -4 8
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14437 None 23 Human Functional pAC50 = 6.1 6.1 6 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 14437 None 23 Human Functional pAC50 = 6.1 6.1 6 4
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2182 None 36 Human Functional pAC50 = 7.1 7.1 -3 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2182 None 36 Human Functional pAC50 = 7.1 7.1 -3 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
3827.0 2182 None 36 Human Functional pAC50 = 7.1 7.1 -3 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2182 None 36 Human Functional pAC50 = 7.1 7.1 -3 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2182 None 36 Human Functional pAC50 = 7.1 7.1 -3 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 2182 None 36 Human Functional pAC50 = 7.1 7.1 -3 25
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 194927 None 32 Human Functional pAC50 = 6.0 6.0 -10 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5311507.0 194927 None 32 Human Functional pAC50 = 6.0 6.0 -10 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 194927 None 32 Human Functional pAC50 = 6.0 6.0 -10 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB01624 194927 None 32 Human Functional pAC50 = 6.0 6.0 -10 12
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 111644 None 40 Human Functional pAC50 = 5.0 5.0 -19 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 111644 None 40 Human Functional pAC50 = 5.0 5.0 -19 23
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 78289 None 22 Human Functional pAC50 = 6.0 6.0 -2 8
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 78289 None 22 Human Functional pAC50 = 6.0 6.0 -2 8
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 3184 None 43 Human Functional pAC50 = 5.0 5.0 -17 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3184 None 43 Human Functional pAC50 = 5.0 5.0 -17 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3184 None 43 Human Functional pAC50 = 5.0 5.0 -17 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
4932.0 3184 None 43 Human Functional pAC50 = 5.0 5.0 -17 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3184 None 43 Human Functional pAC50 = 5.0 5.0 -17 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 3184 None 43 Human Functional pAC50 = 5.0 5.0 -17 13
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 208276 None 49 Human Functional pAC50 = 5.0 5.0 -16 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
5472.0 208276 None 49 Human Functional pAC50 = 5.0 5.0 -16 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 208276 None 49 Human Functional pAC50 = 5.0 5.0 -16 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 208276 None 49 Human Functional pAC50 = 5.0 5.0 -16 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB00208 208276 None 49 Human Functional pAC50 = 5.0 5.0 -16 16
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 110592 None 24 Human Functional pAC50 = 6.0 6.0 -9 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
2780.0 110592 None 24 Human Functional pAC50 = 6.0 6.0 -9 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 110592 None 24 Human Functional pAC50 = 6.0 6.0 -9 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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
DB13511 110592 None 24 Human Functional pAC50 = 6.0 6.0 -9 11
Antagonist activity at human HTR2B in an in vitro cell-based assay 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 187026 None 38 Human Functional pAC50 = 5 5.0 -125 20
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 187026 None 38 Human Functional pAC50 = 5 5.0 -125 20
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 187026 None 38 Human Functional pAC50 = 5 5.0 -125 20
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 None 45 Human Functional pEC50 = 10.2 10.2 -2 26
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 None 45 Human Functional pEC50 = 10.2 10.2 -2 26
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 None 45 Human Functional pEC50 = 10.2 10.2 -2 26
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 None 45 Human Functional pEC50 = 10.2 10.2 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.4 9.4 -2 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -2 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -2 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -2 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -2 26
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 193118 None 4 Human Functional pEC50 = 9.2 9.2 -1 3
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 193118 None 4 Human Functional pEC50 = 9.2 9.2 -1 3
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 193118 None 4 Human Functional pEC50 = 9.2 9.2 -1 3
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 193118 None 4 Human Functional pEC50 = 9.2 9.2 -1 3
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 193118 None 4 Human Functional pEC50 = 9.2 9.2 -1 3
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 193118 None 4 Human Functional pEC50 = 9.2 9.2 -1 3
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.1 9.1 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 120083 None 57 Human Functional pEC50 = 9 9.0 -25 9
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 120083 None 57 Human Functional pEC50 = 9 9.0 -25 9
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 120083 None 57 Human Functional pEC50 = 9 9.0 -25 9
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -2 26
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 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5202 139 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
CHEMBL39 139 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
DB08839 139 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5 139 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5202 139 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
CHEMBL39 139 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
DB08839 139 None 45 Human Functional pEC50 = 8.9 8.9 -2 26
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
439280 120083 None 57 Human Functional pEC50 = 8.9 8.9 -25 9
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 120083 None 57 Human Functional pEC50 = 8.9 8.9 -25 9
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 120083 None 57 Human Functional pEC50 = 8.9 8.9 -25 9
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 192288 None 0 Human Functional pEC50 = 8.9 8.9 -1 3
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 192288 None 0 Human Functional pEC50 = 8.9 8.9 -1 3
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 192288 None 0 Human Functional pEC50 = 8.9 8.9 -1 3
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 192288 None 0 Human Functional pEC50 = 8.9 8.9 -1 3
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -2 26
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 3359 None 19 Human Functional pEC50 = 8.8 8.8 2 5
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 3359 None 19 Human Functional pEC50 = 8.8 8.8 2 5
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 3359 None 19 Human Functional pEC50 = 8.8 8.8 2 5
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
172469352 197023 None 0 Human Functional pEC50 = 8 8.0 57 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5437030 197023 None 0 Human Functional pEC50 = 8 8.0 57 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
4407909 192975 None 0 Human Functional pEC50 = 8 8.0 1 3
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 192975 None 0 Human Functional pEC50 = 8 8.0 1 3
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 192975 None 0 Human Functional pEC50 = 8 8.0 1 3
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 172980 None 0 Human Functional pEC50 = 8 8.0 2 3
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 172980 None 0 Human Functional pEC50 = 8 8.0 2 3
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
168941715 196900 None 0 Human Functional pEC50 = 8.0 8.0 8 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5434434 196900 None 0 Human Functional pEC50 = 8.0 8.0 8 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
4407909 192975 None 0 Human Functional pEC50 = 8.0 8.0 1 3
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 192975 None 0 Human Functional pEC50 = 8.0 8.0 1 3
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 192975 None 0 Human Functional pEC50 = 8.0 8.0 1 3
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 138216 None 0 Human Functional pEC50 = 7 7.0 -1 3
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 138216 None 0 Human Functional pEC50 = 7 7.0 -1 3
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 64130 None 0 Human Functional pEC50 = 7 7.0 -19 3
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 64130 None 0 Human Functional pEC50 = 7 7.0 -19 3
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 63959 None 17 Human Functional pEC50 = 6 6.0 -81 3
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 63959 None 17 Human Functional pEC50 = 6 6.0 -81 3
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 64353 None 37 Human Functional pEC50 = 6 6.0 -89 3
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 64353 None 37 Human Functional pEC50 = 6 6.0 -89 3
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 2412 None 8 Human Functional pEC50 = 6 6.0 -75 4
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 2412 None 8 Human Functional pEC50 = 6 6.0 -75 4
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 2412 None 8 Human Functional pEC50 = 6 6.0 -75 4
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 111735 None 0 Human Functional pEC50 = 6 6.0 -8 2
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 111735 None 0 Human Functional pEC50 = 6 6.0 -8 2
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 138437 None 0 Human Functional pEC50 = 6 6.0 -12 2
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 138437 None 0 Human Functional pEC50 = 6 6.0 -12 2
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 138437 None 0 Human Functional pEC50 = 6 6.0 -12 2
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 2344 None 24 Human Functional pEC50 = 6 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6 6.0 -35 11
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 63321 None 0 Human Functional pEC50 = 6 6.0 -6 2
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 63321 None 0 Human Functional pEC50 = 6 6.0 -6 2
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 63959 None 17 Human Functional pEC50 = 6 6.0 -81 3
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 63959 None 17 Human Functional pEC50 = 6 6.0 -81 3
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
CHEMBL4913232 216564 None 7 Human Functional pEC50 = 6 6.0 -6 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL None None None C1=CC2(CCNCC2)Oc2ccccc21 10.1021/acsmedchemlett.3c00454
122442324 138437 None 0 Human Functional pEC50 = 6 6.0 -12 2
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 138437 None 0 Human Functional pEC50 = 6 6.0 -12 2
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 138437 None 0 Human Functional pEC50 = 6 6.0 -12 2
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 89104 None 0 Human Functional pEC50 = 7 7.0 -23 3
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 89104 None 0 Human Functional pEC50 = 7 7.0 -23 3
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 89104 None 0 Human Functional pEC50 = 7 7.0 -23 3
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 201822 None 0 Human Functional pEC50 = 7 7.0 -6 3
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 201822 None 0 Human Functional pEC50 = 7 7.0 -6 3
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 138447 None 0 Human Functional pEC50 = 7 7.0 -15 3
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 138447 None 0 Human Functional pEC50 = 7 7.0 -15 3
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 138447 None 0 Human Functional pEC50 = 7 7.0 -15 3
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 192983 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192983 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192983 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192983 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192983 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192983 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 138447 None 0 Human Functional pEC50 = 7.0 7.0 -15 3
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 138447 None 0 Human Functional pEC50 = 7.0 7.0 -15 3
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 138447 None 0 Human Functional pEC50 = 7.0 7.0 -15 3
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 189268 None 0 Human Functional pEC50 = 7.0 7.0 6 2
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 189268 None 0 Human Functional pEC50 = 7.0 7.0 6 2
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 192993 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192993 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192993 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192993 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192993 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192993 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 77797 None 4 Human Functional pEC50 = 7.0 7.0 2 3
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 77797 None 4 Human Functional pEC50 = 7.0 7.0 2 3
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 74511 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 74511 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 74511 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
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 183768 None 0 Human Functional pEC50 = 7.0 7.0 -67 3
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 183768 None 0 Human Functional pEC50 = 7.0 7.0 -67 3
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 183768 None 0 Human Functional pEC50 = 7.0 7.0 -67 3
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
168941715 196900 None 0 Human Functional pEC50 = 8.0 8.0 8 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5434434 196900 None 0 Human Functional pEC50 = 8.0 8.0 8 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
5 139 None 45 Human Functional pEC50 = 8.0 8.0 -2 26
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 None 45 Human Functional pEC50 = 8.0 8.0 -2 26
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 None 45 Human Functional pEC50 = 8.0 8.0 -2 26
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 None 45 Human Functional pEC50 = 8.0 8.0 -2 26
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 3982 None 15 Human Functional pEC50 = 8.0 8.0 3 5
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 3982 None 15 Human Functional pEC50 = 8.0 8.0 3 5
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 3982 None 15 Human Functional pEC50 = 8.0 8.0 3 5
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 2069 None 2 Rat Functional pEC50 = 7.9 7.9 2 3
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 2069 None 2 Rat Functional pEC50 = 7.9 7.9 2 3
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 2069 None 2 Rat Functional pEC50 = 7.9 7.9 2 3
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 2069 None 2 Rat Functional pEC50 = 7.9 7.9 2 3
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 2069 None 2 Rat Functional pEC50 = 7.9 7.9 2 3
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 2069 None 2 Rat Functional pEC50 = 7.9 7.9 2 3
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 64353 None 37 Human Functional pEC50 = 6.0 6.0 -89 3
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 64353 None 37 Human Functional pEC50 = 6.0 6.0 -89 3
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 183768 None 0 Human Functional pEC50 = 7.0 7.0 -67 3
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 183768 None 0 Human Functional pEC50 = 7.0 7.0 -67 3
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 183768 None 0 Human Functional pEC50 = 7.0 7.0 -67 3
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 164108 None 0 Human Functional pEC50 = 6.9 6.9 -602 3
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 164108 None 0 Human Functional pEC50 = 6.9 6.9 -602 3
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 56866 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
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 56866 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
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 12564 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
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 12564 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
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 12564 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
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 12706 None 0 Human Functional pEC50 = 6.9 6.9 -8 3
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 12706 None 0 Human Functional pEC50 = 6.9 6.9 -8 3
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 12706 None 0 Human Functional pEC50 = 6.9 6.9 -8 3
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 72077 None 1 Human Functional pEC50 = 5.9 5.9 -11 3
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 72077 None 1 Human Functional pEC50 = 5.9 5.9 -11 3
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 56867 None 0 Human Functional pEC50 = 5.9 5.9 -6 3
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 56867 None 0 Human Functional pEC50 = 5.9 5.9 -6 3
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 12566 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 12566 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 12566 None 0 Human Functional pEC50 = 7.9 7.9 2 3
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 91135 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 91135 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 61479 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 61479 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 187403 None 0 Human Functional pEC50 = 6.9 6.9 -2 2
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 187403 None 0 Human Functional pEC50 = 6.9 6.9 -2 2
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 2011 None 45 Human Functional pEC50 = 6.9 6.9 -5 6
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 193023 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 193023 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 193023 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 62651 None 11 Human Functional pEC50 = 5.9 5.9 -83 3
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 62651 None 11 Human Functional pEC50 = 5.9 5.9 -83 3
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 64330 None 3 Human Functional pEC50 = 5.9 5.9 -407 3
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 64330 None 3 Human Functional pEC50 = 5.9 5.9 -407 3
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 183798 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 183798 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 183798 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 193023 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 193023 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 193023 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 183798 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 183798 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 183798 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 163902 None 0 Human Functional pEC50 = 5.9 5.9 -1000 3
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 163902 None 0 Human Functional pEC50 = 5.9 5.9 -1000 3
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 164894 None 0 Human Functional pEC50 = 5.9 5.9 -1047 2
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 164894 None 0 Human Functional pEC50 = 5.9 5.9 -1047 2
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 12503 None 0 Human Functional pEC50 = 7.9 7.9 -16 3
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 12503 None 0 Human Functional pEC50 = 7.9 7.9 -16 3
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 12503 None 0 Human Functional pEC50 = 7.9 7.9 -16 3
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 56820 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 56820 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 3492 None 32 Human Functional pEC50 = 7.9 7.9 -1 4
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 3492 None 32 Human Functional pEC50 = 7.9 7.9 -1 4
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 3492 None 32 Human Functional pEC50 = 7.9 7.9 -1 4
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 88323 None 0 Rat Functional pEC50 = 6.9 6.9 5 2
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 88323 None 0 Rat Functional pEC50 = 6.9 6.9 5 2
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 63505 None 0 Human Functional pEC50 = 6.9 6.9 -32 3
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 63505 None 0 Human Functional pEC50 = 6.9 6.9 -32 3
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 79139 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 79139 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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
170453288 196449 None 2 Human Functional pEC50 = 7.9 7.9 6 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5424175 196449 None 2 Human Functional pEC50 = 7.9 7.9 6 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
44572168 12488 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 12488 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 12488 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
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 64658 None 0 Human Functional pEC50 = 6.9 6.9 -9 3
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 64658 None 0 Human Functional pEC50 = 6.9 6.9 -9 3
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 62651 None 11 Human Functional pEC50 = 5.9 5.9 -83 3
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 62651 None 11 Human Functional pEC50 = 5.9 5.9 -83 3
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 12705 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
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 12705 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
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 12705 None 0 Human Functional pEC50 = 6.9 6.9 -10 3
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 200920 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 200920 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 56865 None 0 Human Functional pEC50 = 5.8 5.8 -23 3
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 56865 None 0 Human Functional pEC50 = 5.8 5.8 -23 3
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 119060 None 6 Human Functional pEC50 = 5.8 5.8 - 1
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 119060 None 6 Human Functional pEC50 = 5.8 5.8 - 1
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 120720 None 0 Human Functional pEC50 = 5.8 5.8 -1 3
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 120720 None 0 Human Functional pEC50 = 5.8 5.8 -1 3
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 120720 None 0 Human Functional pEC50 = 5.8 5.8 -1 3
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 187400 None 0 Human Functional pEC50 = 7.8 7.8 5 2
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 187400 None 0 Human Functional pEC50 = 7.8 7.8 5 2
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 2860 None 26 Human Functional pEC50 = 7.8 7.8 1 3
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 2860 None 26 Human Functional pEC50 = 7.8 7.8 1 3
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 2860 None 26 Human Functional pEC50 = 7.8 7.8 1 3
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 183772 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 183772 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 183772 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 169307 None 5 Human Functional pEC50 = 5.8 5.8 -158 3
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 169307 None 5 Human Functional pEC50 = 5.8 5.8 -158 3
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 78125 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 78125 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 183772 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 183772 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 183772 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 62548 None 2 Human Functional pEC50 = 5.8 5.8 -239 3
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 62548 None 2 Human Functional pEC50 = 5.8 5.8 -239 3
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
168941654 195567 None 0 Human Functional pEC50 = 7.8 7.8 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
CHEMBL5406172 195567 None 0 Human Functional pEC50 = 7.8 7.8 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
168941654 195567 None 0 Human Functional pEC50 = 7.8 7.8 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
CHEMBL5406172 195567 None 0 Human Functional pEC50 = 7.8 7.8 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
54585653 61485 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 61485 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 84721 None 0 Human Functional pEC50 = 5.8 5.8 -38 3
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 84721 None 0 Human Functional pEC50 = 5.8 5.8 -38 3
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 56821 None 0 Human Functional pEC50 = 6.8 6.8 -53 3
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 56821 None 0 Human Functional pEC50 = 6.8 6.8 -53 3
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 61481 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 61481 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 164506 None 0 Human Functional pEC50 = 6.8 6.8 -1548 2
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 164506 None 0 Human Functional pEC50 = 6.8 6.8 -1548 2
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 138438 None 0 Human Functional pEC50 = 6.8 6.8 -34 3
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 138438 None 0 Human Functional pEC50 = 6.8 6.8 -34 3
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 138438 None 0 Human Functional pEC50 = 6.8 6.8 -34 3
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 120713 None 0 Human Functional pEC50 = 5.8 5.8 -12 2
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 120713 None 0 Human Functional pEC50 = 5.8 5.8 -12 2
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 120713 None 0 Human Functional pEC50 = 5.8 5.8 -12 2
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 187557 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 187557 None 0 Human Functional pEC50 = 7.8 7.8 4 2
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 183796 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
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 183796 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
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 183796 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
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 138435 None 0 Human Functional pEC50 = 5.8 5.8 -54 3
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 138435 None 0 Human Functional pEC50 = 5.8 5.8 -54 3
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 138435 None 0 Human Functional pEC50 = 5.8 5.8 -54 3
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 12531 None 0 Human Functional pEC50 = 5.8 5.8 -5 2
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 12531 None 0 Human Functional pEC50 = 5.8 5.8 -5 2
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 12531 None 0 Human Functional pEC50 = 5.8 5.8 -5 2
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 183796 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
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 183796 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
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 183796 None 0 Human Functional pEC50 = 6.8 6.8 -28 3
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 138435 None 0 Human Functional pEC50 = 5.8 5.8 -54 3
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 138435 None 0 Human Functional pEC50 = 5.8 5.8 -54 3
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 138435 None 0 Human Functional pEC50 = 5.8 5.8 -54 3
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 83524 None 0 Human Functional pEC50 = 6.8 6.8 -15 3
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 83524 None 0 Human Functional pEC50 = 6.8 6.8 -15 3
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 61482 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 61482 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 119061 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 119061 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 172779 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 172779 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
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 192763 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 192763 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 84714 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
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 84714 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
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 183787 None 0 Human Functional pEC50 = 6.8 6.8 -20 3
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 183787 None 0 Human Functional pEC50 = 6.8 6.8 -20 3
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 183787 None 0 Human Functional pEC50 = 6.8 6.8 -20 3
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 123135 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 123135 None 0 Human Functional pEC50 = 6.8 6.8 -6 3
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 62548 None 2 Human Functional pEC50 = 5.8 5.8 -239 3
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 62548 None 2 Human Functional pEC50 = 5.8 5.8 -239 3
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 61477 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 61477 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 12462 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 12462 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 12462 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 202441 None 0 Human Functional pEC50 = 6.7 6.7 -1862 3
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 202441 None 0 Human Functional pEC50 = 6.7 6.7 -1862 3
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
164513426 195281 None 0 Human Functional pEC50 = 6.7 6.7 -4 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 2 2 2.2 C[C@@H]1C=C(c2c[nH]c3ncccc23)CNC1 10.1021/acsmedchemlett.3c00566
CHEMBL5399968 195281 None 0 Human Functional pEC50 = 6.7 6.7 -4 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 2 2 2.2 C[C@@H]1C=C(c2c[nH]c3ncccc23)CNC1 10.1021/acsmedchemlett.3c00566
45485742 200279 None 0 Human Functional pEC50 = 6.7 6.7 -18 3
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 200279 None 0 Human Functional pEC50 = 6.7 6.7 -18 3
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 77810 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 77810 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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
85542158 195546 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
11777150 62625 None 0 Human Functional pEC50 = 6.7 6.7 -63 3
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 62625 None 0 Human Functional pEC50 = 6.7 6.7 -63 3
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
85542158 195546 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
11414184 83531 None 0 Human Functional pEC50 = 6.7 6.7 -7 3
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 83531 None 0 Human Functional pEC50 = 6.7 6.7 -7 3
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 138437 None 0 Human Functional pEC50 = 5.7 5.7 -12 2
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 138437 None 0 Human Functional pEC50 = 5.7 5.7 -12 2
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 138437 None 0 Human Functional pEC50 = 5.7 5.7 -12 2
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 138437 None 0 Human Functional pEC50 = 5.7 5.7 -12 2
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 138437 None 0 Human Functional pEC50 = 5.7 5.7 -12 2
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 138437 None 0 Human Functional pEC50 = 5.7 5.7 -12 2
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 187444 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 187444 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 12466 None 0 Human Functional pEC50 = 6.7 6.7 -7 3
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 12466 None 0 Human Functional pEC50 = 6.7 6.7 -7 3
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 12466 None 0 Human Functional pEC50 = 6.7 6.7 -7 3
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 154787 None 2 Human Functional pEC50 = 6.7 6.7 -3 3
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 154787 None 2 Human Functional pEC50 = 6.7 6.7 -3 3
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 120729 None 0 Human Functional pEC50 = 5.7 5.7 -181 3
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 120729 None 0 Human Functional pEC50 = 5.7 5.7 -181 3
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 120729 None 0 Human Functional pEC50 = 5.7 5.7 -181 3
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 193120 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 193120 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 193120 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 169307 None 5 Human Functional pEC50 = 5.7 5.7 -158 3
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 169307 None 5 Human Functional pEC50 = 5.7 5.7 -158 3
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 193120 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 193120 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 193120 None 0 Human Functional pEC50 = 5.7 5.7 1 2
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 133675 None 29 Rat Functional pEC50 = 8.7 8.7 1 7
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 133675 None 29 Rat Functional pEC50 = 8.7 8.7 1 7
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
5 139 None 45 Human Functional pEC50 = 8.6 8.6 -2 26
Agonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
5202 139 None 45 Human Functional pEC50 = 8.6 8.6 -2 26
Agonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
CHEMBL39 139 None 45 Human Functional pEC50 = 8.6 8.6 -2 26
Agonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
DB08839 139 None 45 Human Functional pEC50 = 8.6 8.6 -2 26
Agonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
166 3359 None 19 Human Functional pEC50 = 8.6 8.6 2 5
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 3359 None 19 Human Functional pEC50 = 8.6 8.6 2 5
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 3359 None 19 Human Functional pEC50 = 8.6 8.6 2 5
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 104936 None 31 Rat Functional pEC50 = 8.6 8.6 1 3
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 104936 None 31 Rat Functional pEC50 = 8.6 8.6 1 3
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 12547 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 12547 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 12547 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 193085 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 193085 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 193085 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 193085 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 193085 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 193085 None 0 Human Functional pEC50 = 6.7 6.7 2 3
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 138088 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 138088 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 89141 None 0 Human Functional pEC50 = 6.7 6.7 -10 3
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 89141 None 0 Human Functional pEC50 = 6.7 6.7 -10 3
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 89141 None 0 Human Functional pEC50 = 6.7 6.7 -10 3
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 138432 None 0 Human Functional pEC50 = 6.7 6.7 -26 3
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 138432 None 0 Human Functional pEC50 = 6.7 6.7 -26 3
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 138432 None 0 Human Functional pEC50 = 6.7 6.7 -26 3
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 138432 None 0 Human Functional pEC50 = 6.7 6.7 -26 3
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 138432 None 0 Human Functional pEC50 = 6.7 6.7 -26 3
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 138432 None 0 Human Functional pEC50 = 6.7 6.7 -26 3
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 12659 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
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 12659 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
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 12659 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
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 2509 None 14 Human Functional pEC50 = 7.7 7.7 -2 17
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 2509 None 14 Human Functional pEC50 = 7.7 7.7 -2 17
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 2509 None 14 Human Functional pEC50 = 7.7 7.7 -2 17
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
8226.0 2509 None 14 Human Functional pEC50 = 7.7 7.7 -2 17
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 2509 None 14 Human Functional pEC50 = 7.7 7.7 -2 17
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 2509 None 14 Human Functional pEC50 = 7.7 7.7 -2 17
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 163774 None 0 Human Functional pEC50 = 7.7 7.7 -19 3
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 163774 None 0 Human Functional pEC50 = 7.7 7.7 -19 3
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 56862 None 0 Human Functional pEC50 = 6.7 6.7 -5 3
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 56862 None 0 Human Functional pEC50 = 6.7 6.7 -5 3
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 56818 None 0 Human Functional pEC50 = 6.7 6.7 -12 3
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 56818 None 0 Human Functional pEC50 = 6.7 6.7 -12 3
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 138429 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 138429 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 138429 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 138429 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 138429 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 138429 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 2344 None 24 Human Functional pEC50 = 6.7 6.7 -35 11
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 2344 None 24 Human Functional pEC50 = 6.7 6.7 -35 11
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 2344 None 24 Human Functional pEC50 = 6.7 6.7 -35 11
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 2344 None 24 Human Functional pEC50 = 6.7 6.7 -35 11
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 2344 None 24 Human Functional pEC50 = 6.7 6.7 -35 11
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 83476 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 83476 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 12464 None 0 Human Functional pEC50 = 7.7 7.7 -7 3
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 12464 None 0 Human Functional pEC50 = 7.7 7.7 -7 3
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 12464 None 0 Human Functional pEC50 = 7.7 7.7 -7 3
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 119062 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 119062 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 207391 None 0 Human Functional pEC50 = 7.7 7.7 2 3
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 207391 None 0 Human Functional pEC50 = 7.7 7.7 2 3
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 61476 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 61476 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 64202 None 0 Human Functional pEC50 = 6.7 6.7 -72 3
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 64202 None 0 Human Functional pEC50 = 6.7 6.7 -72 3
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 120735 None 0 Human Functional pEC50 = 5.7 5.7 -36 2
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 120735 None 0 Human Functional pEC50 = 5.7 5.7 -36 2
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 120735 None 0 Human Functional pEC50 = 5.7 5.7 -36 2
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 12707 None 2 Human Functional pEC50 = 6.7 6.7 -2 2
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 12707 None 2 Human Functional pEC50 = 6.7 6.7 -2 2
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 12707 None 2 Human Functional pEC50 = 6.7 6.7 -2 2
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 56814 None 0 Human Functional pEC50 = 5.7 5.7 -2 3
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 56814 None 0 Human Functional pEC50 = 5.7 5.7 -2 3
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
216 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
9815618 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
CHEMBL253811 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
216 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
9815618 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
CHEMBL253811 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
216 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
9815618 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
CHEMBL253811 2860 None 26 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assayAgonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assay
ChEMBL 203 2 1 1 2.6 C[C@@H](Cc1cccc(c1)C(F)(F)F)N 10.1021/acs.jmedchem.3c01178
44431701 88178 None 0 Rat Functional pEC50 = 7.6 7.6 3 2
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 88178 None 0 Rat Functional pEC50 = 7.6 7.6 3 2
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 74677 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
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 74677 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
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 161972 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
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 161972 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
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 120702 None 1 Human Functional pEC50 = 5.6 5.6 -3 2
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 120702 None 1 Human Functional pEC50 = 5.6 5.6 -3 2
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 120702 None 1 Human Functional pEC50 = 5.6 5.6 -3 2
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 89133 None 0 Human Functional pEC50 = 5.6 5.6 -213 3
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 89133 None 0 Human Functional pEC50 = 5.6 5.6 -213 3
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 89133 None 0 Human Functional pEC50 = 5.6 5.6 -213 3
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 91150 None 0 Human Functional pEC50 = 5.6 5.6 -25 2
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 91150 None 0 Human Functional pEC50 = 5.6 5.6 -25 2
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 193094 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193094 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193094 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 None 16 Rat Functional pEC50 = 6.6 6.6 -123 12
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 None 16 Rat Functional pEC50 = 6.6 6.6 -123 12
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 None 16 Rat Functional pEC50 = 6.6 6.6 -123 12
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 None 16 Rat Functional pEC50 = 6.6 6.6 -123 12
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 111734 None 0 Human Functional pEC50 = 6.6 6.6 -7 2
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 111734 None 0 Human Functional pEC50 = 6.6 6.6 -7 2
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 193092 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193092 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193092 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193094 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193094 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193094 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 138431 None 0 Human Functional pEC50 = 7.6 7.6 -8 3
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 138431 None 0 Human Functional pEC50 = 7.6 7.6 -8 3
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 138431 None 0 Human Functional pEC50 = 7.6 7.6 -8 3
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 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 None 45 Human Functional pEC50 = 7.6 7.6 -2 26
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 193092 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193092 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 193092 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 138431 None 0 Human Functional pEC50 = 7.6 7.6 -8 3
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 138431 None 0 Human Functional pEC50 = 7.6 7.6 -8 3
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 138431 None 0 Human Functional pEC50 = 7.6 7.6 -8 3
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 94909 None 0 Human Functional pEC50 = 6.6 6.6 -31 3
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 94909 None 0 Human Functional pEC50 = 6.6 6.6 -31 3
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 94912 None 1 Human Functional pEC50 = 6.6 6.6 -6 3
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 94912 None 1 Human Functional pEC50 = 6.6 6.6 -6 3
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 130467 None 3 Human Functional pEC50 = 5.6 5.6 -120 3
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 130467 None 3 Human Functional pEC50 = 5.6 5.6 -120 3
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 138436 None 0 Human Functional pEC50 = 5.6 5.6 -8 3
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 138436 None 0 Human Functional pEC50 = 5.6 5.6 -8 3
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 138436 None 0 Human Functional pEC50 = 5.6 5.6 -8 3
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 138436 None 0 Human Functional pEC50 = 5.6 5.6 -8 3
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 138436 None 0 Human Functional pEC50 = 5.6 5.6 -8 3
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 138436 None 0 Human Functional pEC50 = 5.6 5.6 -8 3
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 183741 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183741 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183741 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183769 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 183769 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 183769 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 183741 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183741 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183741 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183769 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 183769 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 183769 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 201414 None 0 Human Functional pEC50 = 6.6 6.6 -8 2
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 201414 None 0 Human Functional pEC50 = 6.6 6.6 -8 2
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 89094 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 89094 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 89094 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183791 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183791 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183791 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183791 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183791 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183791 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 119063 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 119063 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 119066 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 119066 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 138433 None 1 Human Functional pEC50 = 7.6 7.6 -6 3
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 138433 None 1 Human Functional pEC50 = 7.6 7.6 -6 3
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 138433 None 1 Human Functional pEC50 = 7.6 7.6 -6 3
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 138433 None 1 Human Functional pEC50 = 7.6 7.6 -6 3
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 138433 None 1 Human Functional pEC50 = 7.6 7.6 -6 3
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 138433 None 1 Human Functional pEC50 = 7.6 7.6 -6 3
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 202316 None 0 Human Functional pEC50 = 5.6 5.6 -1905 3
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 202316 None 0 Human Functional pEC50 = 5.6 5.6 -1905 3
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 91127 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
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 91127 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
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 12690 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 12690 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 12690 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 84871 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 84871 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 183721 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
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 183721 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
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 183721 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
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
172466550 196777 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
Agonist activity at 5-HT2B (unknown origin)Agonist activity at 5-HT2B (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
CHEMBL5432040 196777 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
Agonist activity at 5-HT2B (unknown origin)Agonist activity at 5-HT2B (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
162643473 183721 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
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 183721 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
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 183721 None 0 Human Functional pEC50 = 6.6 6.6 -14 3
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 141773 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 141773 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 12648 None 0 Human Functional pEC50 = 7.6 7.6 -3 3
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 12648 None 0 Human Functional pEC50 = 7.6 7.6 -3 3
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 12648 None 0 Human Functional pEC50 = 7.6 7.6 -3 3
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 91136 None 0 Human Functional pEC50 = 7.6 7.6 -7 3
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 91136 None 0 Human Functional pEC50 = 7.6 7.6 -7 3
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 137061 None 0 Human Functional pEC50 = 6.6 6.6 -46 3
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 137061 None 0 Human Functional pEC50 = 6.6 6.6 -46 3
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 56815 None 0 Human Functional pEC50 = 5.5 5.5 -4 3
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 56815 None 0 Human Functional pEC50 = 5.5 5.5 -4 3
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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 2011 None 45 Human Functional pEC50 = 6.5 6.5 -5 6
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
172467762 196799 None 0 Human Functional pEC50 = 6.5 6.5 -13 3
Agonist activity at 5HT2B (unknown origin)Agonist activity at 5HT2B (unknown origin)
ChEMBL 235 5 1 2 2.7 NC[C@@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1016/j.bmcl.2024.129654
CHEMBL5432445 196799 None 0 Human Functional pEC50 = 6.5 6.5 -13 3
Agonist activity at 5HT2B (unknown origin)Agonist activity at 5HT2B (unknown origin)
ChEMBL 235 5 1 2 2.7 NC[C@@H]1C[C@@H]1c1cc(F)ccc1OCC1CC1 10.1016/j.bmcl.2024.129654
46937339 74235 None 0 Human Functional pEC50 = 6.5 6.5 -13 3
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 74235 None 0 Human Functional pEC50 = 6.5 6.5 -13 3
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 74235 None 0 Human Functional pEC50 = 6.5 6.5 -13 3
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 74235 None 0 Human Functional pEC50 = 6.5 6.5 -13 3
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 84831 None 0 Human Functional pEC50 = 6.5 6.5 -5 2
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 84831 None 0 Human Functional pEC50 = 6.5 6.5 -5 2
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 137453 None 0 Human Functional pEC50 = 6.5 6.5 -2 3
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 137453 None 0 Human Functional pEC50 = 6.5 6.5 -2 3
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 137327 None 0 Human Functional pEC50 = 5.5 5.5 -208 3
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 137327 None 0 Human Functional pEC50 = 5.5 5.5 -208 3
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 207581 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 207581 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 190079 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 190079 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 190079 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 190079 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 4119 None 22 Human Functional pEC50 = 8.5 8.5 -3 3
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 4119 None 22 Human Functional pEC50 = 8.5 8.5 -3 3
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 4119 None 22 Human Functional pEC50 = 8.5 8.5 -3 3
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 None 45 Rat Functional pEC50 = 8.5 8.5 -7 26
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 None 45 Rat Functional pEC50 = 8.5 8.5 -7 26
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 None 45 Rat Functional pEC50 = 8.5 8.5 -7 26
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 None 45 Rat Functional pEC50 = 8.5 8.5 -7 26
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 12654 None 1 Human Functional pEC50 = 8.4 8.4 -1 3
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 12654 None 1 Human Functional pEC50 = 8.4 8.4 -1 3
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 12654 None 1 Human Functional pEC50 = 8.4 8.4 -1 3
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 16169 None 0 Human Functional pEC50 = 8.4 8.4 -18 2
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 16169 None 0 Human Functional pEC50 = 8.4 8.4 -18 2
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 61483 None 0 Human Functional pEC50 = 7.5 7.5 5 2
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 61483 None 0 Human Functional pEC50 = 7.5 7.5 5 2
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 119065 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119065 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 138444 None 0 Human Functional pEC50 = 7.5 7.5 -30 3
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 138444 None 0 Human Functional pEC50 = 7.5 7.5 -30 3
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 138444 None 0 Human Functional pEC50 = 7.5 7.5 -30 3
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 64904 None 0 Human Functional pEC50 = 7.5 7.5 -6 3
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 64904 None 0 Human Functional pEC50 = 7.5 7.5 -6 3
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 138444 None 0 Human Functional pEC50 = 7.5 7.5 -30 3
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 138444 None 0 Human Functional pEC50 = 7.5 7.5 -30 3
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 138444 None 0 Human Functional pEC50 = 7.5 7.5 -30 3
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 138441 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 138441 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 138441 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 204618 None 0 Human Functional pEC50 = 6.5 6.5 -3019 3
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 204618 None 0 Human Functional pEC50 = 6.5 6.5 -3019 3
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 120709 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 120709 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 120709 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 120715 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 120715 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 120715 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
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 74504 None 0 Human Functional pEC50 = 6.5 6.5 -12 2
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 74504 None 0 Human Functional pEC50 = 6.5 6.5 -12 2
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 74504 None 0 Human Functional pEC50 = 6.5 6.5 -12 2
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 164462 None 0 Human Functional pEC50 = 6.5 6.5 -40 3
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 164462 None 0 Human Functional pEC50 = 6.5 6.5 -40 3
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 183730 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 183730 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 183730 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 183730 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 183730 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 183730 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 12458 None 6 Human Functional pEC50 = 5.5 5.5 -3 2
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 12458 None 6 Human Functional pEC50 = 5.5 5.5 -3 2
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 12458 None 6 Human Functional pEC50 = 5.5 5.5 -3 2
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 89143 None 0 Human Functional pEC50 = 7.5 7.5 -12 3
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 89143 None 0 Human Functional pEC50 = 7.5 7.5 -12 3
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 89143 None 0 Human Functional pEC50 = 7.5 7.5 -12 3
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 138441 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 138441 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 138441 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 207963 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 207963 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 192898 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192898 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192898 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 122838 None 0 Human Functional pEC50 = 6.5 6.5 -51 3
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 122838 None 0 Human Functional pEC50 = 6.5 6.5 -51 3
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 192898 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192898 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192898 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 89160 None 0 Human Functional pEC50 = 7.5 7.5 -9 3
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 89160 None 0 Human Functional pEC50 = 7.5 7.5 -9 3
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 89160 None 0 Human Functional pEC50 = 7.5 7.5 -9 3
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 12441 None 0 Human Functional pEC50 = 7.5 7.5 -6 3
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 12441 None 0 Human Functional pEC50 = 7.5 7.5 -6 3
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 12441 None 0 Human Functional pEC50 = 7.5 7.5 -6 3
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 77762 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 77762 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
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 2344 None 24 Human Functional pEC50 = 6.5 6.5 -35 11
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 2344 None 24 Human Functional pEC50 = 6.5 6.5 -35 11
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 2344 None 24 Human Functional pEC50 = 6.5 6.5 -35 11
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 2344 None 24 Human Functional pEC50 = 6.5 6.5 -35 11
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 2344 None 24 Human Functional pEC50 = 6.5 6.5 -35 11
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 138431 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
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 138431 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
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 138431 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
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 137047 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 137047 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 119064 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 119064 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 187399 None 0 Human Functional pEC50 = 7.5 7.5 -3 2
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 187399 None 0 Human Functional pEC50 = 7.5 7.5 -3 2
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 193155 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 193155 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 193155 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 74484 None 0 Human Functional pEC50 = 6.5 6.5 -18 3
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 74484 None 0 Human Functional pEC50 = 6.5 6.5 -18 3
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 74484 None 0 Human Functional pEC50 = 6.5 6.5 -18 3
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 138431 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
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 138431 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
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 138431 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
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 138430 None 0 Human Functional pEC50 = 5.5 5.5 -51 2
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 138430 None 0 Human Functional pEC50 = 5.5 5.5 -51 2
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 138430 None 0 Human Functional pEC50 = 5.5 5.5 -51 2
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 138430 None 0 Human Functional pEC50 = 5.5 5.5 -51 2
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 138430 None 0 Human Functional pEC50 = 5.5 5.5 -51 2
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 138430 None 0 Human Functional pEC50 = 5.5 5.5 -51 2
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 12674 None 0 Human Functional pEC50 = 5.5 5.5 -38 2
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 12674 None 0 Human Functional pEC50 = 5.5 5.5 -38 2
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 12674 None 0 Human Functional pEC50 = 5.5 5.5 -38 2
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 192902 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192902 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192902 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 183787 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 183787 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 183787 None 0 Human Functional pEC50 = 6.5 6.5 -20 3
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 192902 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192902 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 192902 None 0 Human Functional pEC50 = 6.5 6.5 1 3
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 193155 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 193155 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 193155 None 0 Human Functional pEC50 = 7.5 7.5 2 3
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 174416 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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 174416 None 0 Human Functional pEC50 = 7.5 7.5 2 2
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
22241625 196520 None 0 Human Functional pEC50 = 7.5 7.5 3 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
CHEMBL5425772 196520 None 0 Human Functional pEC50 = 7.5 7.5 3 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
118733766 120703 None 0 Human Functional pEC50 = 5.5 5.5 -33 2
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 120703 None 0 Human Functional pEC50 = 5.5 5.5 -33 2
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 120703 None 0 Human Functional pEC50 = 5.5 5.5 -33 2
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 183865 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 183865 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 183865 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 183865 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 183865 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 183865 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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
22241625 196520 None 0 Human Functional pEC50 = 7.5 7.5 3 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
CHEMBL5425772 196520 None 0 Human Functional pEC50 = 7.5 7.5 3 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
44572757 12653 None 0 Human Functional pEC50 = 6.5 6.5 -7 2
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 12653 None 0 Human Functional pEC50 = 6.5 6.5 -7 2
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 12653 None 0 Human Functional pEC50 = 6.5 6.5 -7 2
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 200974 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 200974 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
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 138438 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 138438 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 138438 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 138438 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 138438 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 138438 None 0 Human Functional pEC50 = 6.5 6.5 -34 3
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 193189 None 0 Human Functional pEC50 = 6.5 6.5 -7 2
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 193189 None 0 Human Functional pEC50 = 6.5 6.5 -7 2
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 193456 None 0 Human Functional pEC50 = 6.5 6.5 -11 2
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 193456 None 0 Human Functional pEC50 = 6.5 6.5 -11 2
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 207931 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 207931 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 122838 None 0 Human Functional pEC50 = 6.4 6.4 -51 3
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 122838 None 0 Human Functional pEC50 = 6.4 6.4 -51 3
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 12647 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 12647 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 12647 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 91126 None 0 Human Functional pEC50 = 7.4 7.4 -12 3
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 91126 None 0 Human Functional pEC50 = 7.4 7.4 -12 3
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 12471 None 5 Human Functional pEC50 = 7.4 7.4 -7 3
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 12471 None 5 Human Functional pEC50 = 7.4 7.4 -7 3
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 12471 None 5 Human Functional pEC50 = 7.4 7.4 -7 3
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 12524 None 0 Human Functional pEC50 = 7.4 7.4 3 3
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 12524 None 0 Human Functional pEC50 = 7.4 7.4 3 3
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 12524 None 0 Human Functional pEC50 = 7.4 7.4 3 3
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 56822 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 56822 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 62519 None 0 Human Functional pEC50 = 6.4 6.4 -83 3
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 62519 None 0 Human Functional pEC50 = 6.4 6.4 -83 3
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 2011 None 45 Human Functional pEC50 = 7.4 7.4 -5 6
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 2011 None 45 Human Functional pEC50 = 7.4 7.4 -5 6
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 2011 None 45 Human Functional pEC50 = 7.4 7.4 -5 6
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 2011 None 45 Human Functional pEC50 = 7.4 7.4 -5 6
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 94880 None 0 Human Functional pEC50 = 7.4 7.4 -10 3
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 94880 None 0 Human Functional pEC50 = 7.4 7.4 -10 3
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 154947 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
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 154947 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
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 202440 None 1 Human Functional pEC50 = 6.4 6.4 -39 3
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 202440 None 1 Human Functional pEC50 = 6.4 6.4 -39 3
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 94910 None 0 Human Functional pEC50 = 6.4 6.4 -50 3
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 94910 None 0 Human Functional pEC50 = 6.4 6.4 -50 3
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 138433 None 1 Human Functional pEC50 = 6.4 6.4 -6 3
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 138433 None 1 Human Functional pEC50 = 6.4 6.4 -6 3
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 138433 None 1 Human Functional pEC50 = 6.4 6.4 -6 3
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 130237 None 20 Human Functional pEC50 = 5.4 5.4 -12 3
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 130237 None 20 Human Functional pEC50 = 5.4 5.4 -12 3
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 207419 None 0 Human Functional pEC50 = 8.4 8.4 1 3
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 207419 None 0 Human Functional pEC50 = 8.4 8.4 1 3
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
152 364 None 24 Rat Functional pEC50 = 8.4 8.4 -2 5
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 364 None 24 Rat Functional pEC50 = 8.4 8.4 -2 5
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 364 None 24 Rat Functional pEC50 = 8.4 8.4 -2 5
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 72737 None 1 Rat Functional pEC50 = 8.4 8.4 1 2
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 72737 None 1 Rat Functional pEC50 = 8.4 8.4 1 2
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 3359 None 19 Human Functional pEC50 = 8.4 8.4 2 5
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 3359 None 19 Human Functional pEC50 = 8.4 8.4 2 5
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 3359 None 19 Human Functional pEC50 = 8.4 8.4 2 5
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 None 45 Human Functional pEC50 = 8.4 8.4 -2 26
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 None 45 Human Functional pEC50 = 8.4 8.4 -2 26
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 None 45 Human Functional pEC50 = 8.4 8.4 -2 26
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 None 45 Human Functional pEC50 = 8.4 8.4 -2 26
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 12652 None 5 Human Functional pEC50 = 8.3 8.3 -3 3
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 12652 None 5 Human Functional pEC50 = 8.3 8.3 -3 3
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 12652 None 5 Human Functional pEC50 = 8.3 8.3 -3 3
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 12550 None 0 Human Functional pEC50 = 8.3 8.3 1 3
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 12550 None 0 Human Functional pEC50 = 8.3 8.3 1 3
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 12550 None 0 Human Functional pEC50 = 8.3 8.3 1 3
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 84827 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
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 84827 None 0 Human Functional pEC50 = 7.4 7.4 -2 3
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 166244 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
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 166244 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
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 138433 None 1 Human Functional pEC50 = 6.4 6.4 -6 3
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 138433 None 1 Human Functional pEC50 = 6.4 6.4 -6 3
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 138433 None 1 Human Functional pEC50 = 6.4 6.4 -6 3
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 63787 None 0 Human Functional pEC50 = 6.4 6.4 -50 3
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 63787 None 0 Human Functional pEC50 = 6.4 6.4 -50 3
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 164150 None 0 Human Functional pEC50 = 5.4 5.4 -323 3
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 164150 None 0 Human Functional pEC50 = 5.4 5.4 -323 3
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 8445 None 0 Human Functional pEC50 = 5.4 5.4 -812 3
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 8445 None 0 Human Functional pEC50 = 5.4 5.4 -812 3
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 12518 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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 12518 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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 12518 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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 61480 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 61480 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 89161 None 0 Human Functional pEC50 = 6.4 6.4 -125 3
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 89161 None 0 Human Functional pEC50 = 6.4 6.4 -125 3
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 89161 None 0 Human Functional pEC50 = 6.4 6.4 -125 3
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 12525 None 0 Human Functional pEC50 = 6.4 6.4 -10 3
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 12525 None 0 Human Functional pEC50 = 6.4 6.4 -10 3
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 12525 None 0 Human Functional pEC50 = 6.4 6.4 -10 3
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 193042 None 0 Human Functional pEC50 = 6.4 6.4 4 3
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 193042 None 0 Human Functional pEC50 = 6.4 6.4 4 3
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 193042 None 0 Human Functional pEC50 = 6.4 6.4 4 3
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 193042 None 0 Human Functional pEC50 = 6.4 6.4 4 3
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 193042 None 0 Human Functional pEC50 = 6.4 6.4 4 3
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 193042 None 0 Human Functional pEC50 = 6.4 6.4 4 3
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 137695 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 137695 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 120717 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 120717 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 120717 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
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 193020 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 193020 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 193020 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 193020 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 193020 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 193020 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 120728 None 0 Human Functional pEC50 = 5.4 5.4 -5 2
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 120728 None 0 Human Functional pEC50 = 5.4 5.4 -5 2
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 120728 None 0 Human Functional pEC50 = 5.4 5.4 -5 2
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 183823 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 183823 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 183823 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 2344 None 24 Human Functional pEC50 = 6.4 6.4 -35 11
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 183823 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 183823 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 183823 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 120736 None 0 Human Functional pEC50 = 5.4 5.4 -12 2
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 120736 None 0 Human Functional pEC50 = 5.4 5.4 -12 2
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 120736 None 0 Human Functional pEC50 = 5.4 5.4 -12 2
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 138430 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
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 138430 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
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 138430 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
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 138430 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
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 138430 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
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 138430 None 0 Human Functional pEC50 = 5.4 5.4 -51 2
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 183821 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 183821 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 183821 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 120718 None 0 Human Functional pEC50 = 5.3 5.3 -4 2
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 120718 None 0 Human Functional pEC50 = 5.3 5.3 -4 2
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 120718 None 0 Human Functional pEC50 = 5.3 5.3 -4 2
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 183845 None 0 Human Functional pEC50 = 6.3 6.3 -21 3
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 183845 None 0 Human Functional pEC50 = 6.3 6.3 -21 3
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 183845 None 0 Human Functional pEC50 = 6.3 6.3 -21 3
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 138434 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 138434 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 138434 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 193114 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 193114 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 193114 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 183845 None 0 Human Functional pEC50 = 6.3 6.3 -21 3
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 183845 None 0 Human Functional pEC50 = 6.3 6.3 -21 3
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 183845 None 0 Human Functional pEC50 = 6.3 6.3 -21 3
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 193114 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 193114 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 193114 None 0 Human Functional pEC50 = 6.3 6.3 1 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -26 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -26 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -26 3
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 138434 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 138434 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 138434 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 12687 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 12687 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 12687 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 183821 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 183821 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 183821 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 201768 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 201768 None 0 Human Functional pEC50 = 7.3 7.3 -25 3
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 120737 None 0 Human Functional pEC50 = 5.3 5.3 -72 3
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 120737 None 0 Human Functional pEC50 = 5.3 5.3 -72 3
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 120737 None 0 Human Functional pEC50 = 5.3 5.3 -72 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -26 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -26 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -26 3
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 138438 None 0 Human Functional pEC50 = 6.3 6.3 -34 3
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 138438 None 0 Human Functional pEC50 = 6.3 6.3 -34 3
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 138438 None 0 Human Functional pEC50 = 6.3 6.3 -34 3
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
57469772 195096 None 1 Human Functional pEC50 = 6.3 6.3 -3 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5396618 195096 None 1 Human Functional pEC50 = 6.3 6.3 -3 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
45484682 200827 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
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 200827 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 187303 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 187303 None 0 Human Functional pEC50 = 6.3 6.3 1 2
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 187404 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 187404 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 164848 None 0 Human Functional pEC50 = 6.3 6.3 -81 3
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 164848 None 0 Human Functional pEC50 = 6.3 6.3 -81 3
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
85542158 195546 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
44412388 78214 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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 78214 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
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
85542158 195546 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
145966293 164549 None 0 Human Functional pEC50 = 6.3 6.3 -14 3
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 164549 None 0 Human Functional pEC50 = 6.3 6.3 -14 3
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 207891 None 0 Human Functional pEC50 = 7.3 7.3 2 3
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 207891 None 0 Human Functional pEC50 = 7.3 7.3 2 3
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 120722 None 0 Human Functional pEC50 = 5.3 5.3 -23 2
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 120722 None 0 Human Functional pEC50 = 5.3 5.3 -23 2
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 120722 None 0 Human Functional pEC50 = 5.3 5.3 -23 2
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 12684 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 12684 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 12684 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 84282 None 4 Human Functional pEC50 = 5.3 5.3 -309 3
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 84282 None 4 Human Functional pEC50 = 5.3 5.3 -309 3
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 83465 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 83465 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 90779 None 28 Human Functional pEC50 = 8.3 8.3 1 3
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 90779 None 28 Human Functional pEC50 = 8.3 8.3 1 3
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 90779 None 28 Human Functional pEC50 = 8.3 8.3 1 3
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 90779 None 28 Human Functional pEC50 = 8.3 8.3 1 3
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 12710 None 0 Human Functional pEC50 = 8.3 8.3 -1 3
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 12710 None 0 Human Functional pEC50 = 8.3 8.3 -1 3
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 12710 None 0 Human Functional pEC50 = 8.3 8.3 -1 3
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
170453288 196449 None 2 Human Functional pEC50 = 8.3 8.3 6 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5424175 196449 None 2 Human Functional pEC50 = 8.3 8.3 6 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
44431688 152829 None 0 Rat Functional pEC50 = 8.2 8.2 1 2
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 152829 None 0 Rat Functional pEC50 = 8.2 8.2 1 2
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 None 45 Human Functional pEC50 = 8.2 8.2 -2 26
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 None 45 Human Functional pEC50 = 8.2 8.2 -2 26
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 None 45 Human Functional pEC50 = 8.2 8.2 -2 26
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 None 45 Human Functional pEC50 = 8.2 8.2 -2 26
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
145 140 None 16 Human Functional pEC50 = 8.2 8.2 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
1832 140 None 16 Human Functional pEC50 = 8.2 8.2 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
CHEMBL7257 140 None 16 Human Functional pEC50 = 8.2 8.2 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
DB14010 140 None 16 Human Functional pEC50 = 8.2 8.2 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
135509961 136216 None 1 Rat Functional pEC50 = 8.2 8.2 -1 2
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 136216 None 1 Rat Functional pEC50 = 8.2 8.2 -1 2
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 62652 None 1 Human Functional pEC50 = 7.3 7.3 -15 3
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 62652 None 1 Human Functional pEC50 = 7.3 7.3 -15 3
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 177531 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 177531 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 85050 None 0 Human Functional pEC50 = 6.3 6.3 -13 3
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 85050 None 0 Human Functional pEC50 = 6.3 6.3 -13 3
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 183327 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 183327 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 64615 None 16 Human Functional pEC50 = 6.3 6.3 -17 3
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 64615 None 16 Human Functional pEC50 = 6.3 6.3 -17 3
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 94935 None 0 Human Functional pEC50 = 6.3 6.3 -63 3
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 94935 None 0 Human Functional pEC50 = 6.3 6.3 -63 3
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 138436 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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 138436 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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 138436 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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
57469772 195096 None 1 Human Functional pEC50 = 6.3 6.3 -3 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
CHEMBL5396618 195096 None 1 Human Functional pEC50 = 6.3 6.3 -3 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1OC1(C=C2)CCNCC1 10.1021/acsmedchemlett.3c00454
24773900 123499 None 6 Human Functional pEC50 = 5.3 5.3 -6 3
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 123499 None 6 Human Functional pEC50 = 5.3 5.3 -6 3
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 120724 None 0 Human Functional pEC50 = 5.3 5.3 -19 2
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 120724 None 0 Human Functional pEC50 = 5.3 5.3 -19 2
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 120724 None 0 Human Functional pEC50 = 5.3 5.3 -19 2
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 56863 None 0 Human Functional pEC50 = 6.3 6.3 -5 3
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 56863 None 0 Human Functional pEC50 = 6.3 6.3 -5 3
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 200283 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 200283 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 138436 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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 138436 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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 138436 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
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 12556 None 0 Human Functional pEC50 = 6.3 6.3 5 2
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 12556 None 0 Human Functional pEC50 = 6.3 6.3 5 2
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 12556 None 0 Human Functional pEC50 = 6.3 6.3 5 2
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 183763 None 0 Human Functional pEC50 = 6.3 6.3 -4 2
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 183763 None 0 Human Functional pEC50 = 6.3 6.3 -4 2
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 183763 None 0 Human Functional pEC50 = 6.3 6.3 -4 2
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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 2344 None 24 Human Functional pEC50 = 6.3 6.3 -35 11
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
172444062 195485 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
CHEMBL5404610 195485 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
11666237 89146 None 0 Human Functional pEC50 = 6.3 6.3 -30 3
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 89146 None 0 Human Functional pEC50 = 6.3 6.3 -30 3
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 89146 None 0 Human Functional pEC50 = 6.3 6.3 -30 3
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 183763 None 0 Human Functional pEC50 = 6.3 6.3 -4 2
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 183763 None 0 Human Functional pEC50 = 6.3 6.3 -4 2
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 183763 None 0 Human Functional pEC50 = 6.3 6.3 -4 2
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
172444062 195485 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
CHEMBL5404610 195485 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
44572755 12463 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
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 12463 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
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 12463 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
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 64615 None 16 Human Functional pEC50 = 6.3 6.3 -17 3
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 64615 None 16 Human Functional pEC50 = 6.3 6.3 -17 3
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 120704 None 0 Human Functional pEC50 = 5.3 5.3 -7 2
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 120704 None 0 Human Functional pEC50 = 5.3 5.3 -7 2
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 120704 None 0 Human Functional pEC50 = 5.3 5.3 -7 2
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 193007 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 193007 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 193007 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 193007 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 193007 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 193007 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 183856 None 0 Human Functional pEC50 = 7.3 7.3 -20 3
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 183856 None 0 Human Functional pEC50 = 7.3 7.3 -20 3
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 183856 None 0 Human Functional pEC50 = 7.3 7.3 -20 3
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 183800 None 0 Human Functional pEC50 = 6.3 6.3 -20 3
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 183800 None 0 Human Functional pEC50 = 6.3 6.3 -20 3
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 183800 None 0 Human Functional pEC50 = 6.3 6.3 -20 3
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 183800 None 0 Human Functional pEC50 = 6.3 6.3 -20 3
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 183800 None 0 Human Functional pEC50 = 6.3 6.3 -20 3
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 183800 None 0 Human Functional pEC50 = 6.3 6.3 -20 3
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 91117 None 0 Human Functional pEC50 = 7.3 7.3 -18 3
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 91117 None 0 Human Functional pEC50 = 7.3 7.3 -18 3
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 202358 None 0 Human Functional pEC50 = 6.3 6.3 -50 3
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 202358 None 0 Human Functional pEC50 = 6.3 6.3 -50 3
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 120712 None 0 Human Functional pEC50 = 5.3 5.3 -2 2
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 120712 None 0 Human Functional pEC50 = 5.3 5.3 -2 2
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 120712 None 0 Human Functional pEC50 = 5.3 5.3 -2 2
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 84261 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 84261 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 3220 None 14 Human Functional pEC50 = 7.2 7.2 1 4
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 3220 None 14 Human Functional pEC50 = 7.2 7.2 1 4
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 3220 None 14 Human Functional pEC50 = 7.2 7.2 1 4
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 183856 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
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 183856 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
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 183856 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
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 193001 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 193001 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 193001 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 183898 None 0 Human Functional pEC50 = 6.2 6.2 -5 2
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 183898 None 0 Human Functional pEC50 = 6.2 6.2 -5 2
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 183898 None 0 Human Functional pEC50 = 6.2 6.2 -5 2
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 193043 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 193043 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 193043 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 183898 None 0 Human Functional pEC50 = 6.2 6.2 -5 2
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 183898 None 0 Human Functional pEC50 = 6.2 6.2 -5 2
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 183898 None 0 Human Functional pEC50 = 6.2 6.2 -5 2
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 193043 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 193043 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 193043 None 0 Human Functional pEC50 = 6.2 6.2 2 2
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 87283 None 0 Rat Functional pEC50 = 7.2 7.2 -13 2
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 87283 None 0 Rat Functional pEC50 = 7.2 7.2 -13 2
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 12657 None 2 Human Functional pEC50 = 7.2 7.2 -5 3
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 12657 None 2 Human Functional pEC50 = 7.2 7.2 -5 3
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 12657 None 2 Human Functional pEC50 = 7.2 7.2 -5 3
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 193001 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 193001 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 193001 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 77827 None 0 Human Functional pEC50 = 7.2 7.2 7 3
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 77827 None 0 Human Functional pEC50 = 7.2 7.2 7 3
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 72079 None 1 Rat Functional pEC50 = 8.2 8.2 -1 2
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 72079 None 1 Rat Functional pEC50 = 8.2 8.2 -1 2
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 145214 None 0 Rat Functional pEC50 = 8.2 8.2 6 2
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 145214 None 0 Rat Functional pEC50 = 8.2 8.2 6 2
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 207392 None 1 Human Functional pEC50 = 8.2 8.2 6 3
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 207392 None 1 Human Functional pEC50 = 8.2 8.2 6 3
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 183755 None 0 Human Functional pEC50 = 7.2 7.2 -22 3
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 183755 None 0 Human Functional pEC50 = 7.2 7.2 -22 3
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 183755 None 0 Human Functional pEC50 = 7.2 7.2 -22 3
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 61484 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 61484 None 0 Human Functional pEC50 = 7.2 7.2 3 2
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 183755 None 0 Human Functional pEC50 = 7.2 7.2 -22 3
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 183755 None 0 Human Functional pEC50 = 7.2 7.2 -22 3
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 183755 None 0 Human Functional pEC50 = 7.2 7.2 -22 3
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 56817 None 0 Human Functional pEC50 = 6.2 6.2 -9 3
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 56817 None 0 Human Functional pEC50 = 6.2 6.2 -9 3
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 138444 None 0 Human Functional pEC50 = 6.2 6.2 -30 3
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 138444 None 0 Human Functional pEC50 = 6.2 6.2 -30 3
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 138444 None 0 Human Functional pEC50 = 6.2 6.2 -30 3
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 138444 None 0 Human Functional pEC50 = 6.2 6.2 -30 3
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 138444 None 0 Human Functional pEC50 = 6.2 6.2 -30 3
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 138444 None 0 Human Functional pEC50 = 6.2 6.2 -30 3
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 120716 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 120716 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 120716 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 201785 None 0 Human Functional pEC50 = 7.2 7.2 -30 4
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 201785 None 0 Human Functional pEC50 = 7.2 7.2 -30 4
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 164186 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 164186 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 61478 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
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 61478 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
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 120706 None 0 Human Functional pEC50 = 5.2 5.2 -4 2
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 120706 None 0 Human Functional pEC50 = 5.2 5.2 -4 2
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 120706 None 0 Human Functional pEC50 = 5.2 5.2 -4 2
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 78331 None 1 Human Functional pEC50 = 7.2 7.2 -2 3
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 78331 None 1 Human Functional pEC50 = 7.2 7.2 -2 3
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 64658 None 0 Human Functional pEC50 = 7.2 7.2 -9 3
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 64658 None 0 Human Functional pEC50 = 7.2 7.2 -9 3
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
149663072 196095 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5416800 196095 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
24773728 94913 None 0 Human Functional pEC50 = 6.2 6.2 -31 3
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 94913 None 0 Human Functional pEC50 = 6.2 6.2 -31 3
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 120719 None 0 Human Functional pEC50 = 6.2 6.2 -19 3
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 120719 None 0 Human Functional pEC50 = 6.2 6.2 -19 3
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 120719 None 0 Human Functional pEC50 = 6.2 6.2 -19 3
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 63337 None 2 Human Functional pEC50 = 7.2 7.2 -32 3
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 63337 None 2 Human Functional pEC50 = 7.2 7.2 -32 3
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 12448 None 1 Human Functional pEC50 = 7.2 7.2 -13 3
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 12448 None 1 Human Functional pEC50 = 7.2 7.2 -13 3
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 12448 None 1 Human Functional pEC50 = 7.2 7.2 -13 3
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 78025 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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 78025 None 0 Human Functional pEC50 = 7.2 7.2 1 3
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
149663072 196095 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
CHEMBL5416800 196095 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 235 0 1 2 2.9 Clc1cccc2c1C=CC1(CCNCC1)O2 10.1021/acsmedchemlett.3c00454
118733796 120705 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 120705 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 120705 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 12709 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 12709 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 12709 None 0 Human Functional pEC50 = 7.2 7.2 -2 2
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 187445 None 0 Human Functional pEC50 = 7.2 7.2 10 2
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 187445 None 0 Human Functional pEC50 = 7.2 7.2 10 2
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 12551 None 0 Human Functional pEC50 = 8.2 8.2 -2 3
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 12551 None 0 Human Functional pEC50 = 8.2 8.2 -2 3
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 12551 None 0 Human Functional pEC50 = 8.2 8.2 -2 3
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 207910 None 0 Human Functional pEC50 = 8.1 8.1 4 3
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 207910 None 0 Human Functional pEC50 = 8.1 8.1 4 3
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 89131 None 0 Human Functional pEC50 = 6.2 6.2 -12 2
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 89131 None 0 Human Functional pEC50 = 6.2 6.2 -12 2
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 89131 None 0 Human Functional pEC50 = 6.2 6.2 -12 2
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 56864 None 0 Human Functional pEC50 = 6.2 6.2 -19 3
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 56864 None 0 Human Functional pEC50 = 6.2 6.2 -19 3
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 138443 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 138443 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 138443 None 0 Human Functional pEC50 = 6.2 6.2 -5 3
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 207980 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 207980 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 183729 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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 183729 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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 183729 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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 183810 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 183810 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 183810 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 138443 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
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 138443 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
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 138443 None 0 Human Functional pEC50 = 6.1 6.1 -5 3
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 183729 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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 183729 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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 183729 None 0 Human Functional pEC50 = 6.1 6.1 -109 3
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 56868 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 56868 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 183810 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 183810 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 183810 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 120723 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 120723 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 120723 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 70324 None 12 Human Functional pEC50 = 7.1 7.1 6 3
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
10624.0 70324 None 12 Human Functional pEC50 = 7.1 7.1 6 3
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 70324 None 12 Human Functional pEC50 = 7.1 7.1 6 3
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 70324 None 12 Human Functional pEC50 = 7.1 7.1 6 3
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
DB11664 70324 None 12 Human Functional pEC50 = 7.1 7.1 6 3
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 202492 None 0 Human Functional pEC50 = 6.1 6.1 -33 3
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 202492 None 0 Human Functional pEC50 = 6.1 6.1 -33 3
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 12658 None 0 Human Functional pEC50 = 7.1 7.1 -4 3
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 12658 None 0 Human Functional pEC50 = 7.1 7.1 -4 3
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 12658 None 0 Human Functional pEC50 = 7.1 7.1 -4 3
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 193166 None 0 Human Functional pEC50 = 7.1 7.1 2 2
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 193166 None 0 Human Functional pEC50 = 7.1 7.1 2 2
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 103095 None 23 Human Functional pEC50 = 7.1 7.1 -3 3
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 103095 None 23 Human Functional pEC50 = 7.1 7.1 -3 3
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 103095 None 23 Human Functional pEC50 = 7.1 7.1 -3 3
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 103095 None 23 Human Functional pEC50 = 7.1 7.1 -3 3
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 103095 None 23 Human Functional pEC50 = 7.1 7.1 -3 3
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 103095 None 23 Human Functional pEC50 = 7.1 7.1 -3 3
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 183799 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 183799 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 183799 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 164501 None 0 Human Functional pEC50 = 6.1 6.1 -6456 3
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 164501 None 0 Human Functional pEC50 = 6.1 6.1 -6456 3
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 183799 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 183799 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 183799 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 12627 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 12627 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 12627 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 183851 None 0 Human Functional pEC50 = 6.1 6.1 -19 3
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 183851 None 0 Human Functional pEC50 = 6.1 6.1 -19 3
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 183851 None 0 Human Functional pEC50 = 6.1 6.1 -19 3
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 164853 None 0 Human Functional pEC50 = 6.1 6.1 -2 3
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 164853 None 0 Human Functional pEC50 = 6.1 6.1 -2 3
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 62652 None 1 Human Functional pEC50 = 7.1 7.1 -15 3
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 62652 None 1 Human Functional pEC50 = 7.1 7.1 -15 3
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 123499 None 6 Human Functional pEC50 = 6.1 6.1 -6 3
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 123499 None 6 Human Functional pEC50 = 6.1 6.1 -6 3
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 183851 None 0 Human Functional pEC50 = 6.1 6.1 -19 3
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 183851 None 0 Human Functional pEC50 = 6.1 6.1 -19 3
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 183851 None 0 Human Functional pEC50 = 6.1 6.1 -19 3
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 2344 None 24 Human Functional pEC50 = 6.1 6.1 -35 11
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 2344 None 24 Human Functional pEC50 = 6.1 6.1 -35 11
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 2344 None 24 Human Functional pEC50 = 6.1 6.1 -35 11
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 2344 None 24 Human Functional pEC50 = 6.1 6.1 -35 11
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 2344 None 24 Human Functional pEC50 = 6.1 6.1 -35 11
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 62519 None 0 Human Functional pEC50 = 6.1 6.1 -83 3
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 62519 None 0 Human Functional pEC50 = 6.1 6.1 -83 3
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 63324 None 2 Human Functional pEC50 = 6.1 6.1 -40 3
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 63324 None 2 Human Functional pEC50 = 6.1 6.1 -40 3
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 94966 None 0 Human Functional pEC50 = 6.1 6.1 -79 3
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 94966 None 0 Human Functional pEC50 = 6.1 6.1 -79 3
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 84872 None 0 Human Functional pEC50 = 8.1 8.1 -5 3
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 84872 None 0 Human Functional pEC50 = 8.1 8.1 -5 3
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
145 140 None 16 Human Functional pEC50 = 8.1 8.1 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
1832 140 None 16 Human Functional pEC50 = 8.1 8.1 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
CHEMBL7257 140 None 16 Human Functional pEC50 = 8.1 8.1 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
DB14010 140 None 16 Human Functional pEC50 = 8.1 8.1 -3 12
Agonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2B receptor expressed in Flp-In-T-REx-293 cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
44572178 12565 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
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 12565 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
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 12565 None 0 Human Functional pEC50 = 8.1 8.1 -1 3
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 72634 None 4 Rat Functional pEC50 = 8.1 8.1 -1 2
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 72634 None 4 Rat Functional pEC50 = 8.1 8.1 -1 2
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 72834 None 1 Rat Functional pEC50 = 8.1 8.1 -1 2
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 72834 None 1 Rat Functional pEC50 = 8.1 8.1 -1 2
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 187304 None 0 Human Functional pEC50 = 6.1 6.1 -17 2
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 187304 None 0 Human Functional pEC50 = 6.1 6.1 -17 2
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 200947 None 0 Human Functional pEC50 = 7.1 7.1 -2 2
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 200947 None 0 Human Functional pEC50 = 7.1 7.1 -2 2
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 84928 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
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 84928 None 0 Human Functional pEC50 = 6.1 6.1 -7 3
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 91152 None 0 Human Functional pEC50 = 6.1 6.1 -10 3
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 91152 None 0 Human Functional pEC50 = 6.1 6.1 -10 3
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 12469 None 0 Human Functional pEC50 = 7.1 7.1 -4 3
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 12469 None 0 Human Functional pEC50 = 7.1 7.1 -4 3
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 12469 None 0 Human Functional pEC50 = 7.1 7.1 -4 3
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 120721 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 120721 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 120721 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 183788 None 0 Human Functional pEC50 = 7.1 7.1 -32 3
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 183788 None 0 Human Functional pEC50 = 7.1 7.1 -32 3
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 183788 None 0 Human Functional pEC50 = 7.1 7.1 -32 3
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 199759 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 199759 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 63324 None 2 Human Functional pEC50 = 6.1 6.1 -40 3
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 63324 None 2 Human Functional pEC50 = 6.1 6.1 -40 3
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 56816 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 56816 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 168866 None 4 Rat Functional pEC50 = 7.1 7.1 1 6
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 168866 None 4 Rat Functional pEC50 = 7.1 7.1 1 6
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 12678 None 15 Human Functional pEC50 = 7.1 7.1 -6 3
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 12678 None 15 Human Functional pEC50 = 7.1 7.1 -6 3
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 12678 None 15 Human Functional pEC50 = 7.1 7.1 -6 3
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 183788 None 0 Human Functional pEC50 = 7.1 7.1 -32 3
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 183788 None 0 Human Functional pEC50 = 7.1 7.1 -32 3
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 183788 None 0 Human Functional pEC50 = 7.1 7.1 -32 3
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 120708 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
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 120708 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
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 120708 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
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 83523 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 83523 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193116 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193116 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193116 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193116 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193116 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 193116 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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
CHEMBL4913232 216564 None 7 Human Functional pEC50 = 6.1 6.1 -6 2
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL None None None C1=CC2(CCNCC2)Oc2ccccc21 10.1021/acsmedchemlett.3c00454
24826868 91116 None 1 Human Functional pEC50 = 8.1 8.1 1 3
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 91116 None 1 Human Functional pEC50 = 8.1 8.1 1 3
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 89105 None 0 Human Functional pEC50 = 8 8.0 -7 3
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 89105 None 0 Human Functional pEC50 = 8 8.0 -7 3
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 89105 None 0 Human Functional pEC50 = 8 8.0 -7 3
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 138449 None 0 Human Functional pEC50 = 6.0 6.0 -9 2
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 138449 None 0 Human Functional pEC50 = 6.0 6.0 -9 2
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 138449 None 0 Human Functional pEC50 = 6.0 6.0 -9 2
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 98073 None 55 Human Functional pEC50 = 7.0 7.0 1 4
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 98073 None 55 Human Functional pEC50 = 7.0 7.0 1 4
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 177531 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 177531 None 0 Human Functional pEC50 = 5.0 5.0 - 1
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 138449 None 0 Human Functional pEC50 = 6.0 6.0 -9 2
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 138449 None 0 Human Functional pEC50 = 6.0 6.0 -9 2
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 138449 None 0 Human Functional pEC50 = 6.0 6.0 -9 2
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 89144 None 0 Human Functional pEC50 = 7.0 7.0 -85 3
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 89144 None 0 Human Functional pEC50 = 7.0 7.0 -85 3
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 89144 None 0 Human Functional pEC50 = 7.0 7.0 -85 3
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 201337 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 201337 None 0 Human Functional pEC50 = 7.0 7.0 -2 2
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 56813 None 0 Human Functional pEC50 = 7.0 7.0 -17 3
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 56813 None 0 Human Functional pEC50 = 7.0 7.0 -17 3
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 56819 None 0 Human Functional pEC50 = 7.0 7.0 -18 3
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 56819 None 0 Human Functional pEC50 = 7.0 7.0 -18 3
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 2344 None 24 Human Functional pEC50 = 6.0 6.0 -35 11
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 138448 None 0 Human Functional pEC50 = 6.0 6.0 -11 3
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 138448 None 0 Human Functional pEC50 = 6.0 6.0 -11 3
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 138448 None 0 Human Functional pEC50 = 6.0 6.0 -11 3
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 138448 None 0 Human Functional pEC50 = 6.0 6.0 -11 3
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 138448 None 0 Human Functional pEC50 = 6.0 6.0 -11 3
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 138448 None 0 Human Functional pEC50 = 6.0 6.0 -11 3
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 193056 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 193056 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 193056 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 192899 None 0 Human Functional pEC50 = 6.0 6.0 -2 3
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 192899 None 0 Human Functional pEC50 = 6.0 6.0 -2 3
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 192899 None 0 Human Functional pEC50 = 6.0 6.0 -2 3
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 192899 None 0 Human Functional pEC50 = 6.0 6.0 -2 3
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 192899 None 0 Human Functional pEC50 = 6.0 6.0 -2 3
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 192899 None 0 Human Functional pEC50 = 6.0 6.0 -2 3
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 193056 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 193056 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 193056 None 0 Human Functional pEC50 = 7.0 7.0 1 3
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 120714 None 0 Human Functional pEC50 = 6 6.0 -10 3
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 120714 None 0 Human Functional pEC50 = 6 6.0 -10 3
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 120714 None 0 Human Functional pEC50 = 6 6.0 -10 3
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 202194 None 0 Human Functional pEC50 = 6 6.0 -8 3
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 202194 None 0 Human Functional pEC50 = 6 6.0 -8 3
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 179395 None 8 Human Functional pIC50 = 9.7 9.7 - 1
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 179395 None 8 Human Functional pIC50 = 9.7 9.7 - 1
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 180675 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 180675 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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
9929424 210338 None 7 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 336 4 2 3 3.9 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)cc1OC 10.1021/acs.jmedchem.3c00734
CHEMBL5419724 210338 None 7 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 336 4 2 3 3.9 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)cc1OC 10.1021/acs.jmedchem.3c00734
CHEMBL96559 210338 None 7 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 336 4 2 3 3.9 COc1ccc(CC2NCCc3c2[nH]c2ccc(C)cc32)cc1OC 10.1021/acs.jmedchem.3c00734
44565831 180542 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 180542 None 0 Human Functional pIC50 = 9.4 9.4 - 1
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 179374 None 0 Human Functional pIC50 = 9.2 9.2 - 1
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 179374 None 0 Human Functional pIC50 = 9.2 9.2 - 1
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 3391 None 49 Human Functional pIC50 = 9.2 9.2 1122 2
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 3391 None 49 Human Functional pIC50 = 9.2 9.2 1122 2
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 3391 None 49 Human Functional pIC50 = 9.2 9.2 1122 2
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 179839 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 179839 None 0 Human Functional pIC50 = 9.0 9.0 - 1
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 80440 None 5 Human Functional pIC50 = 8.7 8.7 - 1
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 80440 None 5 Human Functional pIC50 = 8.7 8.7 - 1
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 189738 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 189738 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 80165 None 9 Human Functional pIC50 = 7 7.0 - 1
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 80165 None 9 Human Functional pIC50 = 7 7.0 - 1
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 163760 None 0 Human Functional pIC50 = 5 5.0 - 1
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 163760 None 0 Human Functional pIC50 = 5 5.0 - 1
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 164769 None 0 Human Functional pIC50 = 5 5.0 - 1
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 164769 None 0 Human Functional pIC50 = 5 5.0 - 1
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 179304 None 0 Human Functional pIC50 = 5 5.0 - 1
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 179304 None 0 Human Functional pIC50 = 5 5.0 - 1
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 136573 None 0 Human Functional pIC50 = 5 5.0 - 1
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 136573 None 0 Human Functional pIC50 = 5 5.0 - 1
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 136595 None 0 Human Functional pIC50 = 5 5.0 - 1
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 136595 None 0 Human Functional pIC50 = 5 5.0 - 1
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 138421 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 138421 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 138376 None 5 Human Functional pIC50 = 6.0 6.0 - 1
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 138376 None 5 Human Functional pIC50 = 6.0 6.0 - 1
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 179401 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 179401 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 189743 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 189743 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 141545 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 141545 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 8080 None 0 Human Functional pIC50 = 6.9 6.9 -21 2
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 8080 None 0 Human Functional pIC50 = 6.9 6.9 -21 2
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 179303 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 179303 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 179373 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 179373 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 171223 None 6 Human Functional pIC50 = 5.9 5.9 - 1
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 171223 None 6 Human Functional pIC50 = 5.9 5.9 - 1
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 179346 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 179346 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 180214 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 180214 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 192329 None 0 Human Functional pIC50 = 5.9 5.9 -8 3
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 192329 None 0 Human Functional pIC50 = 5.9 5.9 -8 3
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 136481 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 136481 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 136558 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 136558 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 136526 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 136526 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 8219 None 0 Human Functional pIC50 = 6.9 6.9 -37 2
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 8219 None 0 Human Functional pIC50 = 6.9 6.9 -37 2
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 138685 None 5 Human Functional pIC50 = 5.9 5.9 - 1
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 138685 None 5 Human Functional pIC50 = 5.9 5.9 - 1
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 3495 None 34 Human Functional pIC50 = 7.9 7.9 - 1
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 3495 None 34 Human Functional pIC50 = 7.9 7.9 - 1
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 3495 None 34 Human Functional pIC50 = 7.9 7.9 - 1
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 87005 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 87005 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 141733 None 5 Human Functional pIC50 = 6.9 6.9 - 1
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 141733 None 5 Human Functional pIC50 = 6.9 6.9 - 1
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 180542 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 180542 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 167331 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 167331 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 139075 None 12 Human Functional pIC50 = 5.8 5.8 - 1
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 139075 None 12 Human Functional pIC50 = 5.8 5.8 - 1
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 139666 None 5 Human Functional pIC50 = 7.8 7.8 - 1
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 139666 None 5 Human Functional pIC50 = 7.8 7.8 - 1
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 179372 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 179372 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 179424 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 179424 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 179324 None 1 Human Functional pIC50 = 5.8 5.8 - 1
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 179324 None 1 Human Functional pIC50 = 5.8 5.8 - 1
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 69776 None 0 Human Functional pIC50 = 5.8 5.8 -154 2
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 69776 None 0 Human Functional pIC50 = 5.8 5.8 -154 2
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 141471 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 141471 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 179399 None 0 Human Functional pIC50 = 4.8 4.8 - 1
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 179399 None 0 Human Functional pIC50 = 4.8 4.8 - 1
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 8176 None 4 Human Functional pIC50 = 6.8 6.8 -21 2
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 8176 None 4 Human Functional pIC50 = 6.8 6.8 -21 2
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 138383 None 26 Human Functional pIC50 = 5.8 5.8 - 1
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 138383 None 26 Human Functional pIC50 = 5.8 5.8 - 1
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 179372 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 179372 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 81081 None 5 Human Functional pIC50 = 6.8 6.8 - 1
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 81081 None 5 Human Functional pIC50 = 6.8 6.8 - 1
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 79958 None 9 Human Functional pIC50 = 6.8 6.8 - 1
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 79958 None 9 Human Functional pIC50 = 6.8 6.8 - 1
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 138348 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 138348 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 167331 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 167331 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 164009 None 0 Human Functional pIC50 = 4.8 4.8 - 1
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 164009 None 0 Human Functional pIC50 = 4.8 4.8 - 1
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 139005 None 5 Human Functional pIC50 = 6.7 6.7 - 1
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 139005 None 5 Human Functional pIC50 = 6.7 6.7 - 1
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 3391 None 49 Human Functional pIC50 = 7.7 7.7 1122 2
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 3391 None 49 Human Functional pIC50 = 7.7 7.7 1122 2
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 3391 None 49 Human Functional pIC50 = 7.7 7.7 1122 2
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 166753 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 166753 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 180674 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 180674 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 171223 None 6 Human Functional pIC50 = 8.6 8.6 - 1
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 171223 None 6 Human Functional pIC50 = 8.6 8.6 - 1
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 179828 None 1 Human Functional pIC50 = 8.6 8.6 - 1
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 179828 None 1 Human Functional pIC50 = 8.6 8.6 - 1
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 189802 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 189802 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 141528 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 141528 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 167465 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 167465 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 179396 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 179396 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 87003 None 0 Human Functional pIC50 = 7.7 7.7 -15 3
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 87003 None 0 Human Functional pIC50 = 7.7 7.7 -15 3
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 167213 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 167213 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 163007 None 1 Human Functional pIC50 = 6.6 6.6 - 1
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 163007 None 1 Human Functional pIC50 = 6.6 6.6 - 1
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 180216 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 180216 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 138290 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 138290 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 138306 None 5 Human Functional pIC50 = 7.6 7.6 - 1
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 138306 None 5 Human Functional pIC50 = 7.6 7.6 - 1
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 189615 None 40 Human Functional pIC50 = 6.6 6.6 - 1
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 189615 None 40 Human Functional pIC50 = 6.6 6.6 - 1
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 202358 None 0 Human Functional pIC50 = 7.6 7.6 -50 3
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 202358 None 0 Human Functional pIC50 = 7.6 7.6 -50 3
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 81104 None 6 Human Functional pIC50 = 6.6 6.6 - 1
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 81104 None 6 Human Functional pIC50 = 6.6 6.6 - 1
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 32401 None 5 Human Functional pIC50 = 6.6 6.6 - 1
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 32401 None 5 Human Functional pIC50 = 6.6 6.6 - 1
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 138396 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 138396 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 80092 None 5 Human Functional pIC50 = 7.5 7.5 - 1
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 80092 None 5 Human Functional pIC50 = 7.5 7.5 - 1
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 181017 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 181017 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 189615 None 40 Human Functional pIC50 = 8.5 8.5 - 1
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 189615 None 40 Human Functional pIC50 = 8.5 8.5 - 1
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 1459 None 23 Human Functional pIC50 = 8.5 8.5 1 4
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 1459 None 23 Human Functional pIC50 = 8.5 8.5 1 4
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 1459 None 23 Human Functional pIC50 = 8.5 8.5 1 4
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 1459 None 23 Human Functional pIC50 = 8.5 8.5 1 4
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 1459 None 23 Human Functional pIC50 = 8.5 8.5 1 4
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 79995 None 7 Human Functional pIC50 = 7.5 7.5 - 1
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 79995 None 7 Human Functional pIC50 = 7.5 7.5 - 1
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 179374 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 179374 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 180674 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 180674 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 191702 None 0 Human Functional pIC50 = 5.5 5.5 -18 3
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 191702 None 0 Human Functional pIC50 = 5.5 5.5 -18 3
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 57339 None 0 Human Functional pIC50 = 4.5 4.5 - 1
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 57339 None 0 Human Functional pIC50 = 4.5 4.5 - 1
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 189743 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 189743 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80022 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80022 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 180675 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 180675 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 181017 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 181017 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 2664 None 5 Human Functional pIC50 = 5.5 5.5 - 1
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 2664 None 5 Human Functional pIC50 = 5.5 5.5 - 1
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 2664 None 5 Human Functional pIC50 = 5.5 5.5 - 1
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 201193 None 5 Human Functional pIC50 = 6.5 6.5 - 1
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 201193 None 5 Human Functional pIC50 = 6.5 6.5 - 1
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 138332 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 138332 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 179347 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 179347 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 179839 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 179839 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 138332 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 138332 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 138333 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 138333 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 80627 None 9 Human Functional pIC50 = 6.5 6.5 - 1
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 80627 None 9 Human Functional pIC50 = 6.5 6.5 - 1
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 87004 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87004 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 164218 None 0 Human Functional pIC50 = 5.4 5.4 3 2
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 164218 None 0 Human Functional pIC50 = 5.4 5.4 3 2
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 136587 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 136587 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 179346 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 179346 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 162096 None 37 Human Functional pIC50 = 5.4 5.4 - 1
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 162096 None 37 Human Functional pIC50 = 5.4 5.4 - 1
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 167004 None 4 Human Functional pIC50 = 6.4 6.4 - 1
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 167004 None 4 Human Functional pIC50 = 6.4 6.4 - 1
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 8081 None 4 Human Functional pIC50 = 6.4 6.4 -60 2
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 8081 None 4 Human Functional pIC50 = 6.4 6.4 -60 2
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 81332 None 5 Human Functional pIC50 = 7.4 7.4 - 1
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 81332 None 5 Human Functional pIC50 = 7.4 7.4 - 1
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 16169 None 0 Human Functional pIC50 = 7.4 7.4 -18 2
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 16169 None 0 Human Functional pIC50 = 7.4 7.4 -18 2
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 190827 None 2 Human Functional pIC50 = 6.4 6.4 - 1
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 190827 None 2 Human Functional pIC50 = 6.4 6.4 - 1
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 191217 None 7 Human Functional pIC50 = 6.4 6.4 - 1
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 191217 None 7 Human Functional pIC50 = 6.4 6.4 - 1
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 191284 None 1 Human Functional pIC50 = 6.4 6.4 - 1
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 191284 None 1 Human Functional pIC50 = 6.4 6.4 - 1
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 192142 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 192142 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 141632 None 7 Human Functional pIC50 = 6.4 6.4 - 1
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 141632 None 7 Human Functional pIC50 = 6.4 6.4 - 1
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 81088 None 5 Human Functional pIC50 = 6.4 6.4 - 1
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 81088 None 5 Human Functional pIC50 = 6.4 6.4 - 1
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 28207 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 28207 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 80454 None 15 Human Functional pIC50 = 7.3 7.3 - 1
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 80454 None 15 Human Functional pIC50 = 7.3 7.3 - 1
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 167388 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 167388 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 82205 None 43 Human Functional pIC50 = 5.3 5.3 - 1
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 82205 None 43 Human Functional pIC50 = 5.3 5.3 - 1
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 180214 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 180214 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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
170792991 196262 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Partial agonist activity at 5-HT2B receptor (unknown origin)Partial agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 351 1 1 5 3.1 Cn1ccc2cc(-n3c(=O)[nH]c4sc5c(c4c3=O)CCCC5)ccc21 10.1021/acs.jmedchem.3c01178
CHEMBL5419983 196262 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Partial agonist activity at 5-HT2B receptor (unknown origin)Partial agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 351 1 1 5 3.1 Cn1ccc2cc(-n3c(=O)[nH]c4sc5c(c4c3=O)CCCC5)ccc21 10.1021/acs.jmedchem.3c01178
2267399 138428 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 138428 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 138316 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 138316 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 79888 None 15 Human Functional pIC50 = 7.3 7.3 - 1
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 79888 None 15 Human Functional pIC50 = 7.3 7.3 - 1
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 80093 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 80093 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 80166 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 80166 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 80348 None 5 Human Functional pIC50 = 5.3 5.3 - 1
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 80348 None 5 Human Functional pIC50 = 5.3 5.3 - 1
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 80550 None 6 Human Functional pIC50 = 5.3 5.3 - 1
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 80550 None 6 Human Functional pIC50 = 5.3 5.3 - 1
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 81082 None 17 Human Functional pIC50 = 5.3 5.3 - 1
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 81082 None 17 Human Functional pIC50 = 5.3 5.3 - 1
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 81504 None 8 Human Functional pIC50 = 5.3 5.3 - 1
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 81504 None 8 Human Functional pIC50 = 5.3 5.3 - 1
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 139072 None 5 Human Functional pIC50 = 5.3 5.3 - 1
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 139072 None 5 Human Functional pIC50 = 5.3 5.3 - 1
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 141549 None 6 Human Functional pIC50 = 5.3 5.3 - 1
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 141549 None 6 Human Functional pIC50 = 5.3 5.3 - 1
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 166072 None 5 Human Functional pIC50 = 5.3 5.3 - 1
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 166072 None 5 Human Functional pIC50 = 5.3 5.3 - 1
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 138388 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 138388 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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
164937988 195320 None 4 Human Functional pIC50 = 6.3 6.3 -19 5
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5400876 195320 None 4 Human Functional pIC50 = 6.3 6.3 -19 5
Antagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT2B receptor (unknown origin) by calcium flux assay
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
3391669 141928 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 141928 None 5 Human Functional pIC50 = 6.3 6.3 - 1
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 189674 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 189674 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 179400 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 179400 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 179302 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 179302 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 82379 None 8 Human Functional pIC50 = 5.2 5.2 -7413 2
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 82379 None 8 Human Functional pIC50 = 5.2 5.2 -7413 2
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 183327 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 183327 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 136624 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 136624 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 3495 None 34 Human Functional pIC50 = 7.2 7.2 - 1
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 3495 None 34 Human Functional pIC50 = 7.2 7.2 - 1
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 3495 None 34 Human Functional pIC50 = 7.2 7.2 - 1
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 179423 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 179423 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 189614 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 189614 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 179395 None 8 Human Functional pIC50 = 8.2 8.2 - 1
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 179395 None 8 Human Functional pIC50 = 8.2 8.2 - 1
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 189802 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 189802 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 179423 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 179423 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 167319 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 167319 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 140216 None 5 Human Functional pIC50 = 6.1 6.1 - 1
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 140216 None 5 Human Functional pIC50 = 6.1 6.1 - 1
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 179828 None 1 Human Functional pIC50 = 7.1 7.1 - 1
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 179828 None 1 Human Functional pIC50 = 7.1 7.1 - 1
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 125107 None 38 Human Functional pIC50 = 5.1 5.1 - 1
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 125107 None 38 Human Functional pIC50 = 5.1 5.1 - 1
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
170793071 196895 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Partial agonist activity at 5-HT2B receptor (unknown origin)Partial agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 443 4 1 7 2.6 CS(=O)(=O)CCn1ccc2cc(-n3c(=O)[nH]c4sc5c(c4c3=O)CCCC5)ccc21 10.1021/acs.jmedchem.3c01178
CHEMBL5434327 196895 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Partial agonist activity at 5-HT2B receptor (unknown origin)Partial agonist activity at 5-HT2B receptor (unknown origin)
ChEMBL 443 4 1 7 2.6 CS(=O)(=O)CCn1ccc2cc(-n3c(=O)[nH]c4sc5c(c4c3=O)CCCC5)ccc21 10.1021/acs.jmedchem.3c01178
3400827 79944 None 8 Human Functional pIC50 = 6.1 6.1 - 1
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 79944 None 8 Human Functional pIC50 = 6.1 6.1 - 1
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 136538 None 0 Human Functional pIC50 = 6.1 6.1 6 3
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 136538 None 0 Human Functional pIC50 = 6.1 6.1 6 3
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 136508 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 136508 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 179304 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 179304 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 164424 None 0 Human Functional pIC50 = 6.1 6.1 8 2
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 164424 None 0 Human Functional pIC50 = 6.1 6.1 8 2
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 189738 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 189738 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 141607 None 5 Human Functional pIC50 = 6.1 6.1 - 1
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 141607 None 5 Human Functional pIC50 = 6.1 6.1 - 1
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 145493 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 145493 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 183392 None 6 Human Functional pIC50 = 5.1 5.1 - 1
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 183392 None 6 Human Functional pIC50 = 5.1 5.1 - 1
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 162642 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 162642 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 189674 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 189674 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 169664 None 17 Human Functional pIC50 = 7.0 7.0 - 1
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 169664 None 17 Human Functional pIC50 = 7.0 7.0 - 1
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 80031 None 5 Human Functional pIC50 = 7.0 7.0 - 1
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 80031 None 5 Human Functional pIC50 = 7.0 7.0 - 1
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 179399 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 179399 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 179400 None 0 Human Functional pIC50 = 6 6.0 - 1
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 179400 None 0 Human Functional pIC50 = 6 6.0 - 1
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 60457 None 6 Rat Functional pKd = 7 7.0 - 0
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 60457 None 6 Rat Functional pKd = 7 7.0 - 0
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 3491 None 49 Rat Functional pKd = 8.0 8.0 - 3
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 3491 None 49 Rat Functional pKd = 8.0 8.0 - 3
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 3491 None 49 Rat Functional pKd = 8.0 8.0 - 3
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 62228 None 2 Rat Functional pKd = 7.9 7.9 - 0
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 62228 None 2 Rat Functional pKd = 7.9 7.9 - 0
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 958 None 57 Rat Functional pKd = 6.9 6.9 - 43
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
135398737.0 958 None 57 Rat Functional pKd = 6.9 6.9 - 43
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
38 958 None 57 Rat Functional pKd = 6.9 6.9 - 43
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
722 958 None 57 Rat Functional pKd = 6.9 6.9 - 43
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 958 None 57 Rat Functional pKd = 6.9 6.9 - 43
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 958 None 57 Rat Functional pKd = 6.9 6.9 - 43
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 120033 None 0 Rat Functional pKd = 6.9 6.9 - 0
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 120033 None 0 Rat Functional pKd = 6.9 6.9 - 0
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 9380 None 0 Rat Functional pKd = 6.9 6.9 - 0
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 9380 None 0 Rat Functional pKd = 6.9 6.9 - 0
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 9380 None 0 Rat Functional pKd = 6.9 6.9 - 0
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 60398 None 7 Rat Functional pKd = 6.9 6.9 - 0
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 60398 None 7 Rat Functional pKd = 6.9 6.9 - 0
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 60456 None 6 Rat Functional pKd = 6.9 6.9 - 0
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 60456 None 6 Rat Functional pKd = 6.9 6.9 - 0
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 60375 None 1 Rat Functional pKd = 6.8 6.8 - 0
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 60375 None 1 Rat Functional pKd = 6.8 6.8 - 0
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 60457 None 6 Rat Functional pKd = 6.8 6.8 - 0
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 60457 None 6 Rat Functional pKd = 6.8 6.8 - 0
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 59711 None 0 Rat Functional pKd = 7.8 7.8 - 0
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 59711 None 0 Rat Functional pKd = 7.8 7.8 - 0
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 9339 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 9339 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 9339 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 15525 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 15525 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 210378 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 210378 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 60480 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 60480 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 8652 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 8652 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 8652 None 0 Rat Functional pKd = 6.8 6.8 - 0
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 958 None 57 Rat Functional pKd = 6.8 6.8 - 43
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
135398737.0 958 None 57 Rat Functional pKd = 6.8 6.8 - 43
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
38 958 None 57 Rat Functional pKd = 6.8 6.8 - 43
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
722 958 None 57 Rat Functional pKd = 6.8 6.8 - 43
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 958 None 57 Rat Functional pKd = 6.8 6.8 - 43
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 958 None 57 Rat Functional pKd = 6.8 6.8 - 43
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 121191 None 0 Rat Functional pKd = 5.7 5.7 - 0
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 121191 None 0 Rat Functional pKd = 5.7 5.7 - 0
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 34696 None 1 Rat Functional pKd = 6.7 6.7 - 0
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 34696 None 1 Rat Functional pKd = 6.7 6.7 - 0
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 34696 None 1 Rat Functional pKd = 6.7 6.7 - 0
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 34696 None 1 Rat Functional pKd = 6.7 6.7 - 0
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 53381 None 0 Rat Functional pKd = 6.7 6.7 - 0
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 53381 None 0 Rat Functional pKd = 6.7 6.7 - 0
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 8661 None 0 Rat Functional pKd = 6.7 6.7 - 0
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 8661 None 0 Rat Functional pKd = 6.7 6.7 - 0
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 8661 None 0 Rat Functional pKd = 6.7 6.7 - 0
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 53288 None 0 Rat Functional pKd = 6.6 6.6 - 0
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 53288 None 0 Rat Functional pKd = 6.6 6.6 - 0
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 34706 None 1 Rat Functional pKd = 6.6 6.6 - 0
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 34706 None 1 Rat Functional pKd = 6.6 6.6 - 0