Ligand source activities (1 row/activity)





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

46780481 107531 20 None 3 15 Human 9.7 pAC50 = 9.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 107531 20 None 3 15 Human 9.7 pAC50 = 9.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 107531 20 None 3 15 Human 9.7 pAC50 = 9.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 107531 20 None 3 15 Human 9.7 pAC50 = 9.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4940 14470 35 None -5 15 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 14470 35 None -5 15 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
16351 102730 47 None -162 17 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 102730 47 None -162 17 Human 6.0 pAC50 = 6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4046 2483 33 None -19 17 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 5.0 pAC50 = 5 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
1427 2013 54 None -933 30 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 54 None -933 30 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 54 None -933 30 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 54 None -933 30 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 54 None -933 30 Human 5.0 pAC50 = 5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2543 3707 68 None -691 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 68 None -691 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 68 None -691 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 68 None -691 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 68 None -691 14 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
2247 505 81 None -23 42 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 81 None -23 42 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 81 None -23 42 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 81 None -23 42 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 81 None -23 42 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
104870 98880 47 None -56 10 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5374 98880 47 None -56 10 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
CHEMBL279085 98880 47 None -56 10 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
4178 195803 63 None -3 2 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 195803 63 None -3 2 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
4046 2483 33 None -19 17 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
54682461 84686 62 None -2 12 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 84686 62 None -2 12 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2520 204008 70 None -10 20 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 204008 70 None -10 20 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 204008 70 None -10 20 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
26987 949 33 None -104 34 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -104 34 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -104 34 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -104 34 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -104 34 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1222 1664 49 None -5 25 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -5 25 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -5 25 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -5 25 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -5 25 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4993 122357 110 None -1 5 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 122357 110 None -1 5 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
242 470 124 None -229 33 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
34 470 124 None -229 33 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 470 124 None -229 33 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 470 124 None -229 33 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 470 124 None -229 33 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
71496458 115564 87 None -3 16 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 115564 87 None -3 16 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
447715 196927 68 None -19 7 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 5 3 3 5.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL566315 196927 68 None -19 7 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 420 5 3 3 5.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1038/s41467-023-40064-9
4452 2762 19 None -85 21 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 19 None -85 21 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 19 None -85 21 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
16363 596 53 None -3 21 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -3 21 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -3 21 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -3 21 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -3 21 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
135398737 958 93 None -6 43 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -6 43 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -6 43 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -6 43 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -6 43 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1385580 29276 76 None -141 19 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29276 76 None -141 19 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29276 76 None -141 19 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
2402 3370 62 None -27 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
216416 111581 48 None -141 23 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 111581 48 None -141 23 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
16960 14487 23 None -1905 7 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1201287 14487 23 None -1905 7 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
4046 2483 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
11504295 2923 47 None -97723 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -97723 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -97723 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -97723 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -97723 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
123606 352 70 None -1071 6 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 70 None -1071 6 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 70 None -1071 6 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 70 None -1071 6 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 70 None -1071 6 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
2333 142335 97 None -14 14 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 142335 97 None -14 14 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
2162 41514 100 None -11 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 41514 100 None -11 22 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
71398 106439 44 None -2290 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 106439 44 None -2290 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
91610 141353 96 None -1 2 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 527 7 2 6 3.5 COc1ccc2c(c1)C(=O)N(CCc1ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc1)C(=O)C2(C)C 10.1038/s41467-023-40064-9
CHEMBL383634 141353 96 None -1 2 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 527 7 2 6 3.5 COc1ccc2c(c1)C(=O)N(CCc1ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc1)C(=O)C2(C)C 10.1038/s41467-023-40064-9
11626560 200937 94 None -6 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 200937 94 None -6 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1212 1662 50 None -14 35 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -14 35 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -14 35 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -14 35 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -14 35 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
212 3806 47 None -141 22 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -141 22 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -141 22 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -141 22 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 47 None -141 22 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4046 2483 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
31101 729 40 None -26 29 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 40 None -26 29 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 40 None -26 29 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 40 None -26 29 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 40 None -26 29 Human 5.9 pAC50 = 5.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
134 2514 24 None -12 18 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 24 None -12 18 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 24 None -12 18 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 24 None -12 18 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 24 None -12 18 Human 6.9 pAC50 = 6.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
1613 2348 53 None -2 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -2 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -2 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -2 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 53 None -2 34 Human 6.9 pAC50 = 6.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1890 2759 49 None -1 24 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -1 24 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -1 24 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -1 24 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 49 None -1 24 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2869 4152 89 None -5011 5 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
60 4152 89 None -5011 5 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
60857 4152 89 None -5011 5 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
CHEMBL1185 4152 89 None -5011 5 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
DB00315 4152 89 None -5011 5 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
31703 194717 63 None -8 8 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 194717 63 None -8 8 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 194717 63 None -8 8 Human 4.9 pAC50 = 4.9 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
21722 17992 31 None -9 21 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 17992 31 None -9 21 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
65700 78260 28 None -41 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2106919 78260 28 None -41 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
3081361 93934 123 None -22 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93934 123 None -22 14 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
135409453 3773 41 None -173 35 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 41 None -173 35 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 41 None -173 35 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
610479 15500 90 None -1 5 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 261 3 2 2 4.1 Cc1c(Cl)cccc1Nc1ccccc1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL121626 15500 90 None -1 5 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 261 3 2 2 4.1 Cc1c(Cl)cccc1Nc1ccccc1C(=O)O 10.1038/s41467-023-40064-9
41684 31221 105 None -33 32 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 31221 105 None -33 32 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2782 32000 67 None -4466 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 32000 67 None -4466 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 32000 67 None -4466 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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
21772 78399 31 None -1000 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
CHEMBL2110816 78399 31 None -1000 10 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
4528 98126 80 None -6 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL273575 98126 80 None -6 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 10.1038/s41467-023-40064-9
1201549 597 24 None -97 26 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 24 None -97 26 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 24 None -97 26 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 24 None -97 26 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 24 None -97 26 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 24 None -97 26 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2342 599 39 None -3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -3 8 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1353 1911 93 None -77 39 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -77 39 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -77 39 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -77 39 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 93 None -77 39 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2583 3776 118 None -8912 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -8912 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -8912 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -8912 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -8912 16 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
124087 1389 114 None -2 27 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 114 None -2 27 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 114 None -2 27 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 114 None -2 27 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 114 None -2 27 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5440 28724 37 None -512 16 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28724 37 None -512 16 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
3926 207241 40 None -2 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 207241 40 None -2 18 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2142 3096 58 None -223 18 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 3096 58 None -223 18 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 3096 58 None -223 18 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 3096 58 None -223 18 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 3096 58 None -223 18 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 3096 58 None -223 18 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5077 3578 79 None -602 13 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 79 None -602 13 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 79 None -602 13 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 79 None -602 13 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 79 None -602 13 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
60606 61560 73 None -7 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 61560 73 None -7 8 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
46199646 120507 69 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 520 8 4 7 3.4 CC(C)(CO)c1cc2cc(NC(=O)C3(c4ccc5c(c4)OC(F)(F)O5)CC3)c(F)cc2n1C[C@@H](O)CO 10.1038/s41467-023-40064-9
CHEMBL3544914 120507 69 None - 1 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 520 8 4 7 3.4 CC(C)(CO)c1cc2cc(NC(=O)C3(c4ccc5c(c4)OC(F)(F)O5)CC3)c(F)cc2n1C[C@@H](O)CO 10.1038/s41467-023-40064-9
5666 102992 35 None -7 5 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 237 5 1 4 1.5 CCOc1ccccc1OCC1CNCCO1 10.1038/s41467-023-40064-9
CHEMBL306700 102992 35 None -7 5 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 237 5 1 4 1.5 CCOc1ccccc1OCC1CNCCO1 10.1038/s41467-023-40064-9
1224 1432 83 None -912 22 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -912 22 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -912 22 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -912 22 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -912 22 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -912 22 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3704 78189 41 None -3 5 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 78189 41 None -3 5 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3198 205513 76 None -29 37 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1201049 205513 76 None -29 37 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL808 205513 76 None -29 37 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
4746 204891 31 None -15 19 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 204891 31 None -15 19 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 204891 31 None -15 19 Human 4.8 pAC50 = 4.8 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
228 445 28 None -316 20 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 28 None -316 20 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 28 None -316 20 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 28 None -316 20 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 28 None -316 20 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
10034073 17161 29 None -3 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 1056 13 7 18 6.2 CCc1c(Cl)c(O)c(Cl)c(O)c1C(=O)O[C@H]1[C@H](O)[C@H](OC)[C@H](OC/C2=C\C=C\C[C@H](O)/C(C)=C/[C@H](CC)[C@@H](O[C@@H]3OC(C)(C)[C@@H](OC(=O)C(C)C)[C@H](O)[C@@H]3O)/C(C)=C/C(C)=C/C[C@@H]([C@@H](C)O)OC2=O)O[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1255800 17161 29 None -3 4 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 1056 13 7 18 6.2 CCc1c(Cl)c(O)c(Cl)c(O)c1C(=O)O[C@H]1[C@H](O)[C@H](OC)[C@H](OC/C2=C\C=C\C[C@H](O)/C(C)=C/[C@H](CC)[C@@H](O[C@@H]3OC(C)(C)[C@@H](OC(=O)C(C)C)[C@H](O)[C@@H]3O)/C(C)=C/C(C)=C/C[C@@H]([C@@H](C)O)OC2=O)O[C@@H]1C 10.1038/s41467-023-40064-9
445643 97389 69 None -2 7 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97389 69 None -2 7 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2378 98687 103 None -34 5 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 4 0 2 5.2 c1ccc(-c2ccc(C(c3ccccc3)n3ccnc3)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL277535 98687 103 None -34 5 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 4 0 2 5.2 c1ccc(-c2ccc(C(c3ccccc3)n3ccnc3)cc2)cc1 10.1038/s41467-023-40064-9
50905713 102396 76 None -1 2 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 416 4 2 6 4.5 C[C@H](Nc1ncnc2nc[nH]c12)c1cc2cccc(Cl)c2c(=O)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3039502 102396 76 None -1 2 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 416 4 2 6 4.5 C[C@H](Nc1ncnc2nc[nH]c12)c1cc2cccc(Cl)c2c(=O)n1-c1ccccc1 10.1038/s41467-023-40064-9
26248 161539 102 None -1 11 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
CHEMBL41286 161539 102 None -1 11 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
47936 193422 88 None -380 6 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 2 3 7 1.5 C=C[C@@]1(C)CC(=O)[C@@]2(O)[C@](C)(O1)[C@@H](OC(C)=O)[C@@H](O)[C@H]1C(C)(C)CC[C@H](O)[C@@]12C 10.1038/s41467-023-40064-9
CHEMBL52606 193422 88 None -380 6 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 410 2 3 7 1.5 C=C[C@@]1(C)CC(=O)[C@@]2(O)[C@](C)(O1)[C@@H](OC(C)=O)[C@@H](O)[C@H]1C(C)(C)CC[C@H](O)[C@@]12C 10.1038/s41467-023-40064-9
2448 99323 70 None -81 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 99323 70 None -81 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4976 203579 29 None -199 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 203579 29 None -199 15 Human 5.8 pAC50 = 5.8 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2713 205271 82 None -3 27 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205271 82 None -3 27 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205271 82 None -3 27 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205271 82 None -3 27 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205271 82 None -3 27 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205271 82 None -3 27 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205271 82 None -3 27 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2855 4132 104 None -9549 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 104 None -9549 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 104 None -9549 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 104 None -9549 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 104 None -9549 12 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5482 14420 80 None -10 13 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1200438 14420 80 None -10 13 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
6127 14499 8 None -117 6 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 14499 8 None -117 6 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3823 50221 42 None -47 15 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50221 42 None -47 15 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50221 42 None -47 15 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2995 204405 53 None -7079 18 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 204405 53 None -7079 18 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 204405 53 None -7079 18 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
154257 178619 67 None -8 19 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 178619 67 None -8 19 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2389 3331 118 None -1 29 Human 8.6 pAC50 = 8.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -1 29 Human 8.6 pAC50 = 8.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -1 29 Human 8.6 pAC50 = 8.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -1 29 Human 8.6 pAC50 = 8.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 118 None -1 29 Human 8.6 pAC50 = 8.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2335 11848 22 None -3 34 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 11848 22 None -3 34 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 11848 22 None -3 34 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 11848 22 None -3 34 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3158 56267 27 None -194 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 56267 27 None -194 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
202 1508 77 None -2 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -2 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -2 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -2 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -2 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3062316 33575 121 None 1 10 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33575 121 None 1 10 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2333 142335 97 None -14 14 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 142335 97 None -14 14 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
11658860 2344 51 None -17 11 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 51 None -17 11 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 51 None -17 11 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 51 None -17 11 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 51 None -17 11 Human 6.7 pAC50 = 6.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
3658 4107 53 None -57 18 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.7 pAC50 = 6.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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
4046 2483 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
47510 172546 39 None -13 3 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 172546 39 None -13 3 Human 4.7 pAC50 = 4.7 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
3949 100614 50 None -22 16 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 100614 50 None -22 16 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
71398 106439 44 None -2290 14 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 106439 44 None -2290 14 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4046 2483 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2351 4300 49 None -9 22 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 4300 49 None -9 22 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 4300 49 None -9 22 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5311017 120604 11 None -32 5 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3545985 120604 11 None -32 5 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
636403 188268 22 None -8 7 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 188268 22 None -8 7 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
48041 107081 46 None 1 6 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 352 6 1 3 4.4 COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1 10.1038/s41467-023-40064-9
CHEMBL315838 107081 46 None 1 6 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 352 6 1 3 4.4 COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1 10.1038/s41467-023-40064-9
213046 2385 59 None -1 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -1 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -1 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -1 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -1 17 Human 7.6 pAC50 = 7.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2136 3095 30 None -45 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 30 None -45 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 30 None -45 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 30 None -45 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 30 None -45 21 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
54454 5258 88 None 1 14 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 5258 88 None 1 14 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3157 1470 71 None -10232 21 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -10232 21 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -10232 21 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -10232 21 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -10232 21 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1830 2590 44 None -416 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 44 None -416 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 44 None -416 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 44 None -416 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 44 None -416 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
10184665 3991 51 None -13489 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 3991 51 None -13489 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 3991 51 None -13489 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 3991 51 None -13489 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 3991 51 None -13489 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
3658 4107 53 None -57 18 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 53 None -57 18 Human 6.6 pAC50 = 6.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
119570 3159 96 None -426 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
2233 3159 96 None -426 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
953 3159 96 None -426 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
CHEMBL301265 3159 96 None -426 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
DB00413 3159 96 None -426 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
9911830 19148 100 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 454 6 2 7 5.6 COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL1289494 19148 100 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 454 6 2 7 5.6 COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC 10.1038/s41467-023-40064-9
68873 43564 64 None -1 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 43564 64 None -1 3 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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
47979 78210 59 None -7943 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 8 2 6 0.7 C=CCN1CCCC1CNC(=O)c1cc(S(N)(=O)=O)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL2105581 78210 59 None -7943 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 383 8 2 6 0.7 C=CCN1CCCC1CNC(=O)c1cc(S(N)(=O)=O)cc(OC)c1OC 10.1038/s41467-023-40064-9
104870 98880 47 None -56 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5374 98880 47 None -56 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
CHEMBL279085 98880 47 None -56 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
4031 99313 28 None -39 12 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
CHEMBL282121 99313 28 None -39 12 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
102 4127 48 None -549 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 48 None -549 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 48 None -549 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 48 None -549 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 48 None -549 20 Human 5.6 pAC50 = 5.6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
45138674 16646 50 None -1 6 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 16646 50 None -1 6 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4011 82408 49 None -46 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 82408 49 None -46 26 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2780 110529 36 None -251 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 110529 36 None -251 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2284 3182 33 None -16 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -16 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -16 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -16 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -16 34 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2286 3183 51 None -20 28 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 51 None -20 28 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 51 None -20 28 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 51 None -20 28 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 51 None -20 28 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
60753 194684 40 None -7 6 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 384 14 2 4 4.2 CCCCCCCN(CC)CCCC(O)c1ccc(NS(C)(=O)=O)cc1 10.1038/s41467-023-40064-9
CHEMBL533 194684 40 None -7 6 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 384 14 2 4 4.2 CCCCCCCN(CC)CCCC(O)c1ccc(NS(C)(=O)=O)cc1 10.1038/s41467-023-40064-9
4942 5718 50 None -31 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 5718 50 None -31 11 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2264 53190 38 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 349 2 1 4 1.5 CN1C(=O)COc2c(C(=O)NC3CN4CCC3CC4)cc(Cl)cc21 10.1038/s41467-023-40064-9
CHEMBL1598608 53190 38 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 349 2 1 4 1.5 CN1C(=O)COc2c(C(=O)NC3CN4CCC3CC4)cc(Cl)cc21 10.1038/s41467-023-40064-9
2351 3286 64 None -457 27 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
2820 3286 64 None -457 27 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
5035 3286 64 None -457 27 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
CHEMBL81 3286 64 None -457 27 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
DB00481 3286 64 None -457 27 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1038/s41467-023-40064-9
5994 4641 88 None -9 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 4641 88 None -9 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
64139 84785 96 None -2 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 0 1 2 4.1 O=C1Nc2ccc(Cl)cc2[C@@](C#CC2CC2)(C(F)(F)F)O1 10.1038/s41467-023-40064-9
CHEMBL223228 84785 96 None -2 9 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 0 1 2 4.1 O=C1Nc2ccc(Cl)cc2[C@@](C#CC2CC2)(C(F)(F)F)O1 10.1038/s41467-023-40064-9
43815 186920 64 None -102 20 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 186920 64 None -102 20 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 186920 64 None -102 20 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5591 157531 90 None -1 17 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 157531 90 None -1 17 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1056 3371 116 None -51 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 116 None -51 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 116 None -51 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 116 None -51 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 116 None -51 10 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
46220502 112583 84 None -91 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 112583 84 None -91 4 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
9417 133512 54 None -346 15 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 133512 54 None -346 15 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 133512 54 None -346 15 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
54684141 208000 82 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 270 2 2 3 3.0 C/C(O)=C(\C#N)C(=O)Nc1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL973 208000 82 None -1 2 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 270 2 2 3 3.0 C/C(O)=C(\C#N)C(=O)Nc1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
2218 15283 23 None -3 12 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15283 23 None -3 12 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
72106 78192 60 None 3 3 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 78192 60 None 3 3 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
25102847 78221 93 None -2 10 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 78221 93 None -2 10 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1210 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 918 51 None -524 22 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
72095 78273 20 None - 1 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 246 6 2 3 1.8 C#CCOc1ccc(N)cc1C(=O)NCCCC 10.1038/s41467-023-40064-9
CHEMBL2107094 78273 20 None - 1 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 246 6 2 3 1.8 C#CCOc1ccc(N)cc1C(=O)NCCCC 10.1038/s41467-023-40064-9
3294 2006 111 None 2 23 Human 8.5 pAC50 = 8.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 111 None 2 23 Human 8.5 pAC50 = 8.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 111 None 2 23 Human 8.5 pAC50 = 8.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 111 None 2 23 Human 8.5 pAC50 = 8.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 111 None 2 23 Human 8.5 pAC50 = 8.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
19675 51670 43 None -4 15 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 51670 43 None -4 15 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2337 3256 77 None -7 29 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -7 29 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -7 29 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -7 29 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 77 None -7 29 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
24826799 10798 104 None 10 20 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 10798 104 None 10 20 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
19861 207523 50 None -10 10 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 207523 50 None -10 10 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2274 3173 58 None -5 36 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -5 36 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -5 36 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -5 36 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -5 36 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1530 2182 50 None -5 25 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -5 25 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -5 25 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -5 25 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 50 None -5 25 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1816 2540 102 None -53 12 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 102 None -53 12 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 102 None -53 12 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 102 None -53 12 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 102 None -53 12 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1209 1658 75 None -3 20 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 75 None -3 20 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 75 None -3 20 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 75 None -3 20 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 75 None -3 20 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5906 14495 23 None -3 4 Human 4.5 pAC50 = 4.5 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 14495 23 None -3 4 Human 4.5 pAC50 = 4.5 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
22323 15299 32 None -2 11 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 15299 32 None -2 11 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 15299 32 None -2 11 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1234 189221 56 None -13 10 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 189221 56 None -13 10 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 189221 56 None -13 10 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2220 3134 82 None 6 17 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 82 None 6 17 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 82 None 6 17 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 82 None 6 17 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 82 None 6 17 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
104850 3330 96 None -323 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 96 None -323 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 96 None -323 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 96 None -323 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 96 None -323 27 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4066 204626 78 None -239 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 204626 78 None -239 16 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2585 803 103 None -724 33 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
522 803 103 None -724 33 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
551 803 103 None -724 33 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 803 103 None -724 33 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 803 103 None -724 33 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
72093 35061 9 None -3 28 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 35061 9 None -3 28 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 35061 9 None -3 28 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2105 3054 37 None -2 25 Human 8.3 pAC50 = 8.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 37 None -2 25 Human 8.3 pAC50 = 8.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 37 None -2 25 Human 8.3 pAC50 = 8.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 37 None -2 25 Human 8.3 pAC50 = 8.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 37 None -2 25 Human 8.3 pAC50 = 8.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
1043 1582 14 None -81 22 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
149 1582 14 None -81 22 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
8223 1582 14 None -81 22 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL442 1582 14 None -81 22 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00696 1582 14 None -81 22 Human 7.4 pAC50 = 7.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
4640 78266 30 None -3 11 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 78266 30 None -3 11 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5453 203619 102 None -93 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 203619 102 None -93 14 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2470 3653 50 None -2570 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 50 None -2570 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 50 None -2570 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 50 None -2570 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 50 None -2570 23 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
2795 14494 37 None 1 4 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 289 5 1 2 3.5 CN(C)CCC(O)(c1ccccc1)c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1201313 14494 37 None 1 4 Human 5.4 pAC50 = 5.4 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 289 5 1 2 3.5 CN(C)CCC(O)(c1ccccc1)c1ccccc1Cl 10.1038/s41467-023-40064-9
25382 9157 37 None -120 21 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 9157 37 None -120 21 Human 5.4 pAC50 = 5.4 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
2407 3372 76 None -138 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 76 None -138 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 76 None -138 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 76 None -138 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 76 None -138 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
2267 559 71 None -190 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -190 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -190 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -190 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 71 None -190 14 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2435 3590 83 None -23 21 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -23 21 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -23 21 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -23 21 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 83 None -23 21 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4150 788 39 None -72 15 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -72 15 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -72 15 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -72 15 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 39 None -72 15 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5329102 194726 86 None -6 37 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 194726 86 None -6 37 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2601 3780 33 None -154 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -154 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -154 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -154 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -154 17 Human 6.3 pAC50 = 6.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
5284550 41721 15 None -251 16 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 41721 15 None -251 16 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2540 4401 111 None -691 28 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 4401 111 None -691 28 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4886 14110 28 None -19 5 Human 4.3 pAC50 = 4.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 293 9 0 4 3.0 CCCCOc1ccc(OCCCN2CCOCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1198 14110 28 None -19 5 Human 4.3 pAC50 = 4.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 293 9 0 4 3.0 CCCCOc1ccc(OCCCN2CCOCC2)cc1 10.1038/s41467-023-40064-9
135398745 2914 112 None -1 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 112 None -1 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 112 None -1 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 112 None -1 33 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1971 2866 38 None -107 32 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 38 None -107 32 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 38 None -107 32 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 38 None -107 32 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 38 None -107 32 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
5311507 194815 41 None -4 12 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 194815 41 None -4 12 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3337 206367 27 None -1 6 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
65801 206367 27 None -1 6 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
66264 206367 27 None -1 6 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
91452 206367 27 None -1 6 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL87493 206367 27 None -1 6 Human 5.3 pAC50 = 5.3 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 10.1038/s41467-023-40064-9
3151 1462 97 None -38 24 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -38 24 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -38 24 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -38 24 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -38 24 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
20628 96548 28 None -1 13 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 96548 28 None -1 13 Human 6.3 pAC50 = 6.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
55645 84370 8 None -3090 11 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 84370 8 None -3090 11 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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
209 3057 97 None -47 14 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -47 14 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -47 14 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -47 14 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 97 None -47 14 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4046 2483 33 None -19 17 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 33 None -19 17 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
9429 202133 58 None -602 18 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 202133 58 None -602 18 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
4450 178228 69 None -9 11 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 178228 69 None -9 11 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1400 1957 70 None -7 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 70 None -7 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 70 None -7 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 70 None -7 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 70 None -7 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 70 None -7 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1343 1889 62 None -112 12 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -112 12 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -112 12 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -112 12 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 62 None -112 12 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
3042 1414 35 None -501 17 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 35 None -501 17 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 35 None -501 17 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 35 None -501 17 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 35 None -501 17 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
37 778 60 None -4 12 Human 7.2 pAC50 = 7.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 60 None -4 12 Human 7.2 pAC50 = 7.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 60 None -4 12 Human 7.2 pAC50 = 7.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 60 None -4 12 Human 7.2 pAC50 = 7.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 60 None -4 12 Human 7.2 pAC50 = 7.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
54841 203127 52 None -3 11 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 203127 52 None -3 11 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
55645 84370 8 None -3090 11 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 84370 8 None -3090 11 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
242 470 124 None -229 33 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
34 470 124 None -229 33 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 470 124 None -229 33 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 470 124 None -229 33 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 470 124 None -229 33 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
2865 4143 73 None 3 20 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 73 None 3 20 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 73 None 3 20 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 73 None 3 20 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 73 None 3 20 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3947 206395 53 None -10 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 206395 53 None -10 16 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
131411 15392 70 None -2 10 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
28446253 15392 70 None -2 10 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
CHEMBL1214598 15392 70 None -2 10 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
168871 89130 14 None -52 13 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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 89130 14 None -52 13 Human 6.2 pAC50 = 6.2 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A 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
2318 154856 29 None -10 15 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 154856 29 None -10 15 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
150 2509 21 None -1 17 Human 8.1 pAC50 = 8.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -1 17 Human 8.1 pAC50 = 8.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -1 17 Human 8.1 pAC50 = 8.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -1 17 Human 8.1 pAC50 = 8.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -1 17 Human 8.1 pAC50 = 8.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
135 2532 43 None -4 33 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 43 None -4 33 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 43 None -4 33 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 43 None -4 33 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 43 None -4 33 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
68867 78173 38 None -1 13 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 78173 38 None -1 13 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2726 919 68 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 68 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 68 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 68 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 68 None -6 42 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
118422671 2757 65 None -2344 23 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 65 None -2344 23 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 65 None -2344 23 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 65 None -2344 23 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 65 None -2344 23 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 65 None -2344 23 Human 5.2 pAC50 = 5.2 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
213 3853 55 None -12 22 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 55 None -12 22 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 55 None -12 22 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 55 None -12 22 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 55 None -12 22 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
44112 121290 48 None -301 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 121290 48 None -301 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2402 3370 62 None -27 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 62 None -27 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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
2762 3863 31 None -234 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
5587 3863 31 None -234 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
7318 3863 31 None -234 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL1241 3863 31 None -234 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
DB00792 3863 31 None -234 9 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
3936 52488 94 None -4 2 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 328 3 0 4 3.8 COc1cccc(N(C)C(=S)Oc2ccc3c(c2)CCCC3)n1 10.1038/s41467-023-40064-9
CHEMBL1591365 52488 94 None -4 2 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 328 3 0 4 3.8 COc1cccc(N(C)C(=S)Oc2ccc3c(c2)CCCC3)n1 10.1038/s41467-023-40064-9
2169 44847 35 None -128 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 44847 35 None -128 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
214 3860 58 None -7 28 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -7 28 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -7 28 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -7 28 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -7 28 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -7 28 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2393 3334 82 None -128 9 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 82 None -128 9 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 82 None -128 9 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 82 None -128 9 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 82 None -128 9 Human 5.1 pAC50 = 5.1 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
191 403 98 None 1 36 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 98 None 1 36 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 98 None 1 36 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 98 None 1 36 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 98 None 1 36 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
103 4153 61 None -3 22 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 61 None -3 22 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 61 None -3 22 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 61 None -3 22 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 61 None -3 22 Human 7.1 pAC50 = 7.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2477 745 59 None -173 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -173 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -173 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -173 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 59 None -173 20 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
1024 1289 71 None -141 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None None 10.1038/s41467-023-40064-9
162639143 1289 71 None -141 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None None 10.1038/s41467-023-40064-9
5284373 1289 71 None -141 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None None 10.1038/s41467-023-40064-9
760 1289 71 None -141 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL160 1289 71 None -141 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB00091 1289 71 None -141 5 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL None None None None 10.1038/s41467-023-40064-9
3191 102858 97 None -48 33 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102858 97 None -48 33 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
17676 7072 29 None -199 13 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 7072 29 None -199 13 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 7072 29 None -199 13 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4046 2483 33 None -19 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 33 None -19 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
441074 19414 82 None -4 11 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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 19414 82 None -4 11 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based 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
2398 954 62 None -123 36 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 62 None -123 36 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 62 None -123 36 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 62 None -123 36 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 62 None -123 36 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
180 401 56 None -158 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 56 None -158 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 56 None -158 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 56 None -158 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 56 None -158 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
4418 34222 85 None -165 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 34222 85 None -165 18 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3149 12614 15 None 3 26 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 12614 15 None 3 26 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
65981 18454 102 None 2 3 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 452 10 2 4 5.2 CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N2CCCCC2)ccc1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1272 18454 102 None 2 3 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 452 10 2 4 5.2 CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N2CCCCC2)ccc1C(=O)O 10.1038/s41467-023-40064-9
5803 162227 84 None -2 8 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 162227 84 None -2 8 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
100 3805 58 None -6 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -6 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -6 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -6 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 58 None -6 38 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
2895 203592 41 None -9 15 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 203592 41 None -9 15 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
3689 102771 55 None -1380 16 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 102771 55 None -1380 16 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 102771 55 None -1380 16 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
65709 59881 39 None -4 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1729803 59881 39 None -4 13 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
124 2981 47 None -177 24 Human 7.0 pAC50 = 7.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 47 None -177 24 Human 7.0 pAC50 = 7.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 47 None -177 24 Human 7.0 pAC50 = 7.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 47 None -177 24 Human 7.0 pAC50 = 7.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 47 None -177 24 Human 7.0 pAC50 = 7.0 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
68617 205527 62 None -14 30 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205527 62 None -14 30 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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 205527 62 None -14 30 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR2A 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
10531 1420 21 None -100 25 Human 6.0 pAC50 = 6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -100 25 Human 6.0 pAC50 = 6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -100 25 Human 6.0 pAC50 = 6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -100 25 Human 6.0 pAC50 = 6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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 21 None -100 25 Human 6.0 pAC50 = 6 Functional
Agonist activity at human HTR2A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR2A in an in vitro cell-based 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
5 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 72 None -19 26 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168289382 191793 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198213 191793 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168289382 191793 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5198213 191793 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 4 4 2.8 COc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
107 141 121 None 6309 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.bmcl.2014.07.062
1833 141 121 None 6309 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.bmcl.2014.07.062
CHEMBL8165 141 121 None 6309 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1016/j.bmcl.2014.07.062
5 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 139 72 None -19 26 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
5202 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
CHEMBL39 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
DB08839 139 72 None 2 26 Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.9b01061
11247569 199420 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL591223 199420 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
1524 2181 96 None 1 18 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
197 2181 96 None 1 18 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
3822 2181 96 None 1 18 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
88 2181 96 None 1 18 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
CHEMBL51 2181 96 None 1 18 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
DB12465 2181 96 None 1 18 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2013.02.020
5 139 72 None -19 26 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5202 139 72 None -19 26 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
CHEMBL39 139 72 None -19 26 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
DB08839 139 72 None -19 26 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT2A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
439280 120019 107 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 120019 107 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 120019 107 None -9 9 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1021/acs.jmedchem.5b01153
5 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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
168291775 191906 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5200026 191906 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168291775 191906 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5200026 191906 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
5 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5202 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
CHEMBL39 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
DB08839 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2013.03.066
5 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
5202 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
CHEMBL39 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
DB08839 139 72 None -19 26 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
4376990 193009 5 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193009 5 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193009 5 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193009 5 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193009 5 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193009 5 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
145 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
1832 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
CHEMBL7257 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
DB14010 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.2c00129
145 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
1832 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
CHEMBL7257 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
DB14010 140 49 None 6 11 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.1c00577
5 139 72 None -19 26 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
5202 139 72 None -19 26 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
CHEMBL39 139 72 None -19 26 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm5019274
DB08839 139 72 None -19 26 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120019 107 None -9 9 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 120019 107 None -9 9 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 120019 107 None -9 9 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
152743520 189979 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 326 8 1 5 2.9 COc1cc(CCNCc2ccccc2OC)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5170895 189979 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 326 8 1 5 2.9 COc1cc(CCNCc2ccccc2OC)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
11695000 89071 0 None -17 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89071 0 None -17 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89071 0 None -17 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
24773649 94827 0 None -2 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 94827 0 None -2 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
122180957 121772 0 None 20 2 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assayPartial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assay
ChEMBL 393 7 1 5 3.5 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
CHEMBL3589578 121772 0 None 20 2 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assayPartial agonist activity at human 5-HT2A receptor expressed in human tsA201 cells after 30 mins by inositol phosphate turnover assay
ChEMBL 393 7 1 5 3.5 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1Br 10.1016/j.bmc.2014.12.011
10105208 62499 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 62499 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
17954204 63938 23 None -7 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
CHEMBL180668 63938 23 None -7 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 181 0 1 1 2.0 Clc1ccc2c(c1)CCNCC2 10.1021/jm0709034
24773816 94856 0 None -12 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 94856 0 None -12 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
23395431 94913 0 None -10 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 94913 0 None -10 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
24773650 154697 2 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
CHEMBL399750 154697 2 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 225 1 1 2 2.6 COc1cc2c(cc1Cl)CCNCC2C 10.1021/jm0709034
10105208 62499 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 62499 0 None -15 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
22368315 63766 0 None -12 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 63766 0 None -12 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
9994008 166149 0 None -9 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 166149 0 None -9 3 Human 7.0 pEC50 = 7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
96783829 192802 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay
ChEMBL 218 2 2 1 2.6 Fc1cccc2[nH]cc(C[C@H]3CCCN3)c12 10.1021/acsmedchemlett.2c00128
CHEMBL5174204 192802 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay
ChEMBL 218 2 2 1 2.6 Fc1cccc2[nH]cc(C[C@H]3CCCN3)c12 10.1021/acsmedchemlett.2c00128
CHEMBL5221436 192802 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay
ChEMBL 218 2 2 1 2.6 Fc1cccc2[nH]cc(C[C@H]3CCCN3)c12 10.1021/acsmedchemlett.2c00128
24773897 94858 3 None -251 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 C[C@@H]1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
CHEMBL253807 94858 3 None -251 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 213 0 1 1 2.7 C[C@@H]1CNCCc2ccc(Cl)c(F)c21 10.1021/jm0709034
134265705 164091 0 None -1621 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164091 0 None -1621 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
134265590 164758 0 None -309 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164758 0 None -309 3 Human 4.0 pEC50 = 4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
118733794 120673 0 None -15 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120673 0 None -15 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120673 0 None -15 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
118733818 120665 0 None -93 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120665 0 None -93 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120665 0 None -93 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
24826871 91112 0 None -85 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397907 91112 0 None -85 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
157114558 192864 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5187568 192864 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221884 192864 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
24826963 91115 0 None -74 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397910 91115 0 None -74 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 0 1 2 1.3 Cc1cc(C)c2c(c1)C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
11176570 91120 1 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397915 91120 1 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2cc(C(F)(F)F)ccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
157114558 192864 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5187568 192864 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221884 192864 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1O 10.1021/acsmedchemlett.1c00694
18735309 205433 0 None -21 3 Human 6.0 pEC50 = 6.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 205433 0 None -21 3 Human 6.0 pEC50 = 6.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
24826787 91097 0 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397892 91097 0 None -6 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 270 0 1 2 1.7 O=C1c2c(cccc2C(F)(F)F)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
122442268 138353 0 None -7 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769633 138353 0 None -7 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771389 138353 0 None -7 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
168276822 190123 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 324 6 1 5 2.8 COc1cc(CCNC2COc3ccccc32)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5173321 190123 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 324 6 1 5 2.8 COc1cc(CCNC2COc3ccccc32)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
44412405 77781 0 None -5 3 Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 77781 0 None -5 3 Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
122442268 138353 0 None -7 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769633 138353 0 None -7 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771389 138353 0 None -7 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 255 5 1 2 3.1 C=CCOc1ccc(Cl)c(F)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
58911579 91096 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397891 91096 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 242 1 1 2 1.5 O=C1c2c(cccc2C2CC2)C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
162644827 183623 0 None -16 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183623 0 None -16 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183623 0 None -16 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162644827 183623 0 None -16 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183623 0 None -16 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183623 0 None -16 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162657367 183682 0 None -42 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183682 0 None -42 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183682 0 None -42 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
45485781 197391 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 368 5 1 6 1.8 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.07.136
CHEMBL569342 197391 0 None -23 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 368 5 1 6 1.8 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.07.136
5 139 72 None -19 26 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
5202 139 72 None -19 26 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
CHEMBL39 139 72 None -19 26 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2003.05.001
DB08839 139 72 None -19 26 Human 8.0 pEC50 = 8.0 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
122180976 121791 2 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 379 8 1 4 3.8 COc1cccc(CNCCc2cc(OC)c(Br)cc2OC)c1 10.1021/acs.jmedchem.2c00702
CHEMBL3589597 121791 2 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 379 8 1 4 3.8 COc1cccc(CNCCc2cc(OC)c(Br)cc2OC)c1 10.1021/acs.jmedchem.2c00702
122180977 121792 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 365 7 2 4 3.5 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL3589598 121792 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 365 7 2 4 3.5 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5080051 214662 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL None None None Oc1cccc2[nH]cc(CCN3CCC3)c12 10.1021/acsmedchemlett.2c00129
3906894 101979 24 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
CHEMBL301466 101979 24 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
10401602 123069 0 None -3 3 Human 7.0 pEC50 = 7.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 123069 0 None -3 3 Human 7.0 pEC50 = 7.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
44383397 59242 0 None -6 2 Human 6.0 pEC50 = 6.0 Functional
Functional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 246 3 1 2 3.1 CNCCc1cn2c3c(cc(F)cc13)CCC2C 10.1016/s0960-894x(00)00141-4
CHEMBL170319 59242 0 None -6 2 Human 6.0 pEC50 = 6.0 Functional
Functional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional antagonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 246 3 1 2 3.1 CNCCc1cn2c3c(cc(F)cc13)CCC2C 10.1016/s0960-894x(00)00141-4
11437171 83490 0 None -2 3 Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 83490 0 None -2 3 Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
162657367 183682 0 None -42 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183682 0 None -42 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183682 0 None -42 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
168272608 192793 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192793 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192793 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
162670523 183750 0 None -41 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183750 0 None -41 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183750 0 None -41 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
44412404 77768 6 None -10 3 Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 77768 6 None -10 3 Human 6.0 pEC50 = 6.0 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
168272608 192793 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192793 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192793 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
162670523 183750 0 None -41 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183750 0 None -41 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183750 0 None -41 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
45485779 197507 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.8 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
CHEMBL570023 197507 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 348 5 1 6 1.8 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2Cl)n1 10.1016/j.bmcl.2009.07.136
168282376 192886 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5189339 192886 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222002 192886 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168282376 192886 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5189339 192886 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222002 192886 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
24849050 78300 2 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 78300 2 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
162659049 183693 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183693 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183693 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162659049 183693 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183693 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183693 0 None -13 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
11302765 84248 4 None -74 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 84248 4 None -74 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
122442251 138360 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
3906894 101979 24 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
CHEMBL301466 101979 24 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 271 0 2 3 1.7 O=C1Nc2cc(Cl)c(Cl)cc2N2CCNCC12 10.1021/jm301656h
5 139 72 None -19 26 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
5202 139 72 None -19 26 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
CHEMBL39 139 72 None -19 26 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
DB08839 139 72 None -19 26 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
CHEMBL4790446 214071 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4803723 214071 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4790446 214071 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL4803723 214071 2 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
1621 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
17 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
5761 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
CHEMBL263881 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
DB04829 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
46233391 199200 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 454 4 2 4 5.4 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)c1 10.1021/jm9007328
CHEMBL589769 199200 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 454 4 2 4 5.4 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)c1 10.1021/jm9007328
168280534 192868 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5183493 192868 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5221899 192868 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
168280534 192868 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5183493 192868 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
CHEMBL5221899 192868 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 4.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1C(F)(F)F 10.1021/acsmedchemlett.1c00694
122442251 138360 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
107992 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
72197306 102488 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
CHEMBL2393231 102488 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
CHEMBL3040287 102488 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 276 2 2 6 -0.0 CNc1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
107992 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 49 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
118733762 120644 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120644 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120644 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
53324327 56850 0 None -2 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56850 0 None -2 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
16115517 84838 0 None -87 3 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 84838 0 None -87 3 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
11206703 91092 0 None -40 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 91092 0 None -40 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
168268736 192789 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192789 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192789 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168268736 192789 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192789 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192789 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
57799306 89109 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89109 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89109 0 None -47 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
9881119 205473 0 None -4 3 Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 205473 0 None -4 3 Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
5 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
5202 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
CHEMBL39 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0709034
DB08839 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
11160564 63304 4 None -7 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 63304 4 None -7 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
11608308 64309 4 None -42 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 64309 4 None -42 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
24773809 94882 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 94882 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
3991761 192896 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183437 192896 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222058 192896 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
728636 114304 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 188 3 2 1 2.4 CC[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
CHEMBL3330646 114304 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 188 3 2 1 2.4 CC[C@@H](N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
16115388 137366 0 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 137366 0 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
3991761 192896 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183437 192896 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222058 192896 2 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 2 3.6 COc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
11514226 89110 0 None -114 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89110 0 None -114 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89110 0 None -114 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
11609026 89127 0 None -38 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89127 0 None -38 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89127 0 None -38 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
71562661 87307 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 87307 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
1621 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
17 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
5761 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
CHEMBL263881 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
DB04829 2429 17 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.2c00702
439280 120019 107 None -9 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/j.bmcl.2015.07.030
6971044 120019 107 None -9 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/j.bmcl.2015.07.030
CHEMBL350221 120019 107 None -9 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAgonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 220 3 4 3 0.8 N[C@@H](Cc1c[nH]c2ccc(O)cc12)C(=O)O 10.1016/j.bmcl.2015.07.030
46884102 8062 1 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
CHEMBL1091106 8062 1 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 366 5 2 3 3.7 CC1(C)CCC(Oc2cc(F)c(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
5 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
5202 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
CHEMBL39 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
DB08839 139 72 None -19 26 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.2c00702
46230099 199312 0 None -70 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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 199312 0 None -70 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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
71562661 87307 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 87307 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
118733808 120656 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120656 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120656 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
11414184 83498 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 83498 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
166 3359 18 None -36 4 Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 18 None -36 4 Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 18 None -36 4 Human 6.9 pEC50 = 6.9 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
134265622 164753 0 None -223 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164753 0 None -223 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
46228422 200036 0 None -60 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 200036 0 None -60 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
168277051 192837 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5178562 192837 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221669 192837 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168277051 192837 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5178562 192837 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221669 192837 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 362 2 2 2 5.2 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(Cl)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168295524 193030 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5205848 193030 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222868 193030 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
168276542 190312 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5176147 190312 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
168295524 193030 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5205848 193030 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222868 193030 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 2 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
168280316 192863 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5187275 192863 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221883 192863 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
168280316 192863 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5187275 192863 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221883 192863 0 None -41 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.8 Clc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
11608308 64309 4 None -42 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL181076 64309 4 None -42 3 Human 6.9 pEC50 = 6.9 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 C[C@@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
71681897 91119 0 None -87 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
CHEMBL2397914 91119 0 None -87 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 258 0 1 3 1.0 O=C1c2ccc3c(c2C[C@@H]2CNCCN12)OCCC3 10.1016/j.bmcl.2013.04.061
53324165 56801 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56801 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
9901086 187631 33 None -95 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 187631 33 None -95 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
168290116 192964 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5193251 192964 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222481 192964 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
168290116 192964 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5193251 192964 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222481 192964 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 292 3 3 2 3.7 Oc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
44572657 12467 6 None -263 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12467 6 None -263 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12467 6 None -263 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
12370465 12674 18 None -109 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL1187354 12674 18 None -109 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
CHEMBL500093 12674 18 None -109 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 147 2 1 1 1.7 NCC1CC1c1ccccc1 10.1021/jm801354e
9901086 187631 33 None -95 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 187631 33 None -95 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
168288579 192943 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5197871 192943 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222382 192943 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
168288579 192943 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5197871 192943 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222382 192943 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 3.8 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
11949706 200055 0 None -1445 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
CHEMBL595645 200055 0 None -1445 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 359 4 1 4 3.4 C[C@@H]1CNCCN1c1ccc2c(n1)[C@@H](OCc1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.10.112
16743289 59569 3 None -724 2 Human 6.8 pEC50 = 6.8 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
CHEMBL171774 59569 3 None -724 2 Human 6.8 pEC50 = 6.8 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 200 2 1 2 2.1 NCCc1cn2c3c(cccc13)CCC2 10.1016/s0960-894x(00)00141-4
168283046 192892 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192892 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192892 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
5 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
168283046 192892 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192892 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192892 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
118733806 120655 0 None -46 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120655 0 None -46 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120655 0 None -46 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
24826957 91117 0 None -24 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397912 91117 0 None -24 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 246 1 1 3 1.0 COc1ccc(C)c2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
44572804 12623 1 None -48 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12623 1 None -48 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12623 1 None -48 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
CHEMBL4757837 214068 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802974 214068 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4757837 214068 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802974 214068 1 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
5 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 72 None -19 26 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
7153 98020 77 None -1 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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 98020 77 None -1 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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
22292784 64594 15 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 64594 15 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
11952353 199860 0 None -1071 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 199860 0 None -1071 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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
168268703 192776 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5170024 192776 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221265 192776 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
168268703 192776 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5170024 192776 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221265 192776 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 338 1 2 2 5.3 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
122442263 138357 0 None -15 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
46884137 8442 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 352 5 2 3 3.3 C[C@H]1CC[C@@H](Oc2c(F)cc(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
CHEMBL1093698 8442 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 352 5 2 3 3.3 C[C@H]1CC[C@@H](Oc2c(F)cc(CNC(=O)[C@@H]3CCCN3)cc2F)CC1 10.1016/j.bmcl.2010.01.107
72197481 102402 0 None 4 2 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL2393240 102402 0 None 4 2 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL3039632 102402 0 None 4 2 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 356 3 2 6 1.8 CN1CCN(c2nc3c(c(Nc4ccc(F)cc4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
168280955 192875 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5184449 192875 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221926 192875 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
168280955 192875 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5184449 192875 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221926 192875 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cc2ccccc2s1 10.1021/acsmedchemlett.1c00694
168288855 192948 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5194467 192948 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5222402 192948 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
11658860 2344 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
22292784 64594 15 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
CHEMBL181672 64594 15 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2cc(Cl)ccc21 10.1021/jm0709034
168280043 192859 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5188736 192859 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221859 192859 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
3568612 192995 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5203138 192995 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222646 192995 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
10329912 62551 8 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1021/jm0709034
CHEMBL178252 62551 8 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1021/jm0709034
24773979 130169 21 None -4 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
CHEMBL367796 130169 21 None -4 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1021/jm0709034
24773978 154416 1 None -7 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 0 1 1 2.8 CC1(C)CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL398926 154416 1 None -7 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 209 0 1 1 2.8 CC1(C)CNCCc2ccc(Cl)cc21 10.1021/jm0709034
168288855 192948 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5194467 192948 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5222402 192948 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 314 1 4 3 3.5 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Cl)ccc1O 10.1021/acsmedchemlett.1c00694
168280043 192859 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5188736 192859 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221859 192859 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
9991444 62632 1 None -4 3 Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 62632 1 None -4 3 Human 7.8 pEC50 = 7.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
3568612 192995 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5203138 192995 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222646 192995 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
45484663 198368 0 None - 1 Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nnc2c3c(nc(Cc4ccccc4)n12)CCNCC3 10.1016/j.bmcl.2009.07.063
CHEMBL576631 198368 0 None - 1 Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nnc2c3c(nc(Cc4ccccc4)n12)CCNCC3 10.1016/j.bmcl.2009.07.063
10329912 62551 8 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL178252 62551 8 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 179 0 1 1 2.1 CC1CNCCc2ccc(F)cc21 10.1016/j.bmcl.2004.12.080
24773979 130169 21 None -4 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1016/j.bmcl.2004.12.080
CHEMBL367796 130169 21 None -4 3 Human 5.8 pEC50 = 5.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 161 0 1 1 1.9 CC1CNCCc2ccccc21 10.1016/j.bmcl.2004.12.080
44572755 12459 1 None -70 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12459 1 None -70 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12459 1 None -70 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
11427139 84687 0 None -38 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 84687 0 None -38 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
44315993 172877 0 None -16 3 Human 6.8 pEC50 = 6.8 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 172877 0 None -16 3 Human 6.8 pEC50 = 6.8 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
168288743 192947 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192947 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192947 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
11658860 2344 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442273 138356 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138356 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138356 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
118733824 120669 0 None -75 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416065 120669 0 None -75 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546960 120669 0 None -75 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 239 5 1 2 2.8 C=C(F)COc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
16115654 136974 0 None -27 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 136974 0 None -27 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
168288743 192947 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192947 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192947 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
1355 2011 88 None -4 6 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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 88 None -4 6 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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 88 None -4 6 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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 88 None -4 6 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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
122442273 138356 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138356 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138356 0 None -1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
11630623 89099 0 None -151 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89099 0 None -151 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89099 0 None -151 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
44572749 12437 1 None -32 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12437 1 None -32 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12437 1 None -32 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168290300 191986 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 314 7 1 4 3.0 COc1cc(CCNCc2ccccc2F)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5201317 191986 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 314 7 1 4 3.0 COc1cc(CCNCc2ccccc2F)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
11983273 77996 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 77996 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
25084025 12701 1 None -117 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12701 1 None -117 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12701 1 None -117 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168280082 191193 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 340 7 1 6 2.6 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5189232 191193 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 340 7 1 6 2.6 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
122442263 138357 0 None -15 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
11160564 63304 4 None -7 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 63304 4 None -7 3 Human 6.8 pEC50 = 6.8 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
168276542 190312 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5176147 190312 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 391 6 1 4 4.1 COc1cc(CCNC2CCOc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
11221167 84680 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 84680 0 None -25 3 Human 6.8 pEC50 = 6.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
168268771 192791 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5174331 192791 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221385 192791 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
168268771 192791 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5174331 192791 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221385 192791 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 322 1 2 2 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Cl)s1 10.1021/acsmedchemlett.1c00694
11737032 85016 0 None -47 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 85016 0 None -47 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
145709 114302 25 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 194 2 2 1 2.3 NCCc1c[nH]c2c(Cl)cccc12 10.1016/j.bmcl.2014.07.062
CHEMBL3330643 114302 25 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 194 2 2 1 2.3 NCCc1c[nH]c2c(Cl)cccc12 10.1016/j.bmcl.2014.07.062
1534 103040 53 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 103040 53 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 103040 53 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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
44622849 196791 0 None - 1 Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
CHEMBL565547 196791 0 None - 1 Dog 5.8 pEC50 = 5.8 Functional
Agonist activity at 5-HT2A receptor in dog bladder stripAgonist activity at 5-HT2A receptor in dog bladder strip
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
44315697 205505 0 None -8 3 Human 6.7 pEC50 = 6.7 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 205505 0 None -8 3 Human 6.7 pEC50 = 6.7 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
118733810 120657 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120657 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120657 0 None -19 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
3568128 192933 1 None -4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192933 1 None -4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192933 1 None -4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192933 1 None -4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192933 1 None -4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192933 1 None -4 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
11716185 89064 0 None -70 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337497 89064 0 None -70 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2364998 89064 0 None -70 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 CCc1cc(Cl)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
44572800 12653 3 None -190 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12653 3 None -190 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12653 3 None -190 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
9822580 200520 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 404 3 2 3 5.1 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(Cl)cc2)c1 10.1021/jm9007328
CHEMBL598808 200520 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 404 3 2 3 5.1 Cn1ncc(Br)c1-c1cccc(NC(=O)Nc2ccc(Cl)cc2)c1 10.1021/jm9007328
14107683 178126 22 None -2 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
CHEMBL4648350 178126 22 None -2 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
1534 103040 53 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 103040 53 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 103040 53 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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
14107683 178126 22 None -2 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
CHEMBL4648350 178126 22 None -2 2 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
9991444 62632 1 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 62632 1 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
11658860 2344 51 None -17 11 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 51 None -17 11 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 51 None -17 11 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 51 None -17 11 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 51 None -17 11 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
168295545 193044 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.3 Fc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5205884 193044 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.3 Fc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222933 193044 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.3 Fc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
168295545 193044 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.3 Fc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5205884 193044 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.3 Fc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222933 193044 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 5.3 Fc1ccc2[nH]c3c(c2c1)CCNC3C(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.1c00694
44573004 12520 1 None -52 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12520 1 None -52 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12520 1 None -52 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
58911582 91099 0 None -16 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397894 91099 0 None -16 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 232 1 1 3 0.7 COc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
3071387 192770 1 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5172342 192770 1 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221228 192770 1 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
3939391 192950 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5197949 192950 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222415 192950 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
162656326 183677 0 None -6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4757142 183677 0 None -6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802987 183677 0 None -6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
3071387 192770 1 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5172342 192770 1 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221228 192770 1 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 216 1 3 2 2.5 CCC1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
3939391 192950 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5197949 192950 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222415 192950 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccc2ccccc2c1 10.1021/acsmedchemlett.1c00694
162656326 183677 0 None -6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4757142 183677 0 None -6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802987 183677 0 None -6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@@H]1C[C@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
216 2860 32 None -12 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 32 None -12 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 32 None -12 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
11447552 62528 4 None -30 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 62528 4 None -30 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
10465263 64332 63 None -19 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
CHEMBL181172 64332 63 None -19 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 195 0 1 1 2.6 CC1CNCCc2ccc(Cl)cc21 10.1021/jm0709034
24773895 94857 0 None -25 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 94857 0 None -25 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
152 364 29 None -1 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1016/j.bmcl.2018.04.059
2107 364 29 None -1 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1016/j.bmcl.2018.04.059
CHEMBL275854 364 29 None -1 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1016/j.bmcl.2018.04.059
5 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5202 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
CHEMBL39 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
DB08839 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01194
5 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
5202 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
CHEMBL39 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
DB08839 139 72 None -19 26 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm301656h
146 135 85 None 851 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 10.1016/j.bmcl.2014.07.062
164682 135 85 None 851 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 10.1016/j.bmcl.2014.07.062
CHEMBL275628 135 85 None 851 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 10.1016/j.bmcl.2014.07.062
90489020 190873 9 None 14 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2ccccc2O)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5184791 190873 9 None 14 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2ccccc2O)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
50878551 90745 61 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 90745 61 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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
156836209 188575 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 220 4 1 1 2.8 CCN(C)CCc1c[nH]c2ccc(F)cc12 10.1021/acsmedchemlett.1c00577
CHEMBL4873240 188575 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 220 4 1 1 2.8 CCN(C)CCc1c[nH]c2ccc(F)cc12 10.1021/acsmedchemlett.1c00577
CHEMBL5028766 188575 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 220 4 1 1 2.8 CCN(C)CCc1c[nH]c2ccc(F)cc12 10.1021/acsmedchemlett.1c00577
122442260 138354 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442263 138357 0 None -15 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
53317924 56851 0 None -10 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56851 0 None -10 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
58911534 91109 0 None -7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
CHEMBL2397904 91109 0 None -7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C[C@@H]1CNCCN1C2=O 10.1016/j.bmcl.2013.04.061
4646586 193013 2 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5209080 193013 2 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222774 193013 2 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168268773 192792 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177208 192792 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221390 192792 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
4401618 193023 5 None 9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207633 193023 5 None 9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222820 193023 5 None 9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
27559 203409 11 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 203409 11 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
168268773 192792 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177208 192792 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221390 192792 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1cccc(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
4646586 193013 2 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5209080 193013 2 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222774 193013 2 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 2 4.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
4401618 193023 5 None 9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207633 193023 5 None 9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222820 193023 5 None 9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 2 1 3.9 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
11595191 89060 0 None -51 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89060 0 None -51 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89060 0 None -51 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
23492 114300 60 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 1 2 1.7 Cn1cc(CCN)c2ccccc21 10.1016/j.bmcl.2014.07.062
CHEMBL3330641 114300 60 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 1 2 1.7 Cn1cc(CCN)c2ccccc21 10.1016/j.bmcl.2014.07.062
57799324 89092 0 None -9 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2337501 89092 0 None -9 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
CHEMBL2365359 89092 0 None -9 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 Cc1ccc2c(c1Cl)C(=O)N[C@H]1CNC[C@H]21 10.1016/j.bmcl.2012.10.091
122442260 138354 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
27559 203409 11 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 203409 11 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
122442286 138351 0 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
146025686 183759 0 None -21 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183759 0 None -21 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183759 0 None -21 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183759 0 None -21 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183759 0 None -21 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183759 0 None -21 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
122442286 138351 0 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
168294789 193036 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(F)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5208018 193036 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(F)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5222900 193036 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(F)ccc1O 10.1021/acsmedchemlett.1c00694
44572759 12462 1 None -83 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12462 1 None -83 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12462 1 None -83 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168294789 193036 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(F)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5208018 193036 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(F)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5222900 193036 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(F)ccc1O 10.1021/acsmedchemlett.1c00694
146025688 183694 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183694 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183694 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
24826867 91095 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397890 91095 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 230 1 1 2 1.2 CCc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
146025687 183715 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183715 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183715 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
10472780 63283 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 345 3 1 2 4.3 CC1CNCCc2cc(OCc3ccccc3)c(Br)cc21 10.1016/j.bmcl.2004.12.080
CHEMBL179244 63283 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 345 3 1 2 4.3 CC1CNCCc2cc(OCc3ccccc3)c(Br)cc21 10.1016/j.bmcl.2004.12.080
141 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.2c00129
6089 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.2c00129
CHEMBL12420 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.2c00129
DB01488 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.2c00129
141 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.1c00577
6089 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.1c00577
CHEMBL12420 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.1c00577
DB01488 1427 35 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.1c00577
146025687 183715 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183715 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183715 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
16115513 136402 0 None -43 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
CHEMBL373531 136402 0 None -43 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL 252 1 1 3 1.4 COc1ccc(Cl)c2c1[C@@H]1CNCCN1C2=O 10.1021/jm0612968
11447552 62528 4 None -30 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 62528 4 None -30 3 Human 6.7 pEC50 = 6.7 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
44412150 77733 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 77733 0 None -1 3 Human 6.7 pEC50 = 6.7 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
46228433 199740 8 None -87 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 217 1 1 3 1.4 c1cc2c(nc1N1CCNCC1)CCCC2 10.1016/j.bmcl.2009.10.112
CHEMBL593547 199740 8 None -87 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 217 1 1 3 1.4 c1cc2c(nc1N1CCNCC1)CCCC2 10.1016/j.bmcl.2009.10.112
146025688 183694 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183694 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183694 0 None -81 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
168274581 192814 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5176473 192814 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221497 192814 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
168274581 192814 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5176473 192814 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221497 192814 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 280 1 4 3 2.8 Oc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
168285159 192914 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192914 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192914 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168285159 192914 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192914 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192914 0 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
27559 203409 11 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 203409 11 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
168273192 190416 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5177900 190416 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
168297263 192412 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 377 6 1 4 3.7 COc1cc(CCNC2COc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5208046 192412 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 377 6 1 4 3.7 COc1cc(CCNC2COc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
1534 103040 53 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
9287 103040 53 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
CHEMBL30713 103040 53 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
27559 203409 11 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
CHEMBL6557 203409 11 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 200 0 1 2 1.9 Cn1c2c(c3ccccc31)CCNCC2 10.1021/jm301656h
168273192 190416 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5177900 190416 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
168297263 192412 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 377 6 1 4 3.7 COc1cc(CCNC2COc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL5208046 192412 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 377 6 1 4 3.7 COc1cc(CCNC2COc3ccccc32)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
53321947 56798 0 None -3 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56798 0 None -3 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
146025685 183659 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752976 183659 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802794 183659 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
122442293 138342 0 None -20 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138342 0 None -20 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138342 0 None -20 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442250 138344 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
146025685 183659 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4752976 183659 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
CHEMBL4802794 183659 0 None -19 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL 251 5 1 3 2.0 NC[C@H]1C[C@@H]1c1c(OCCF)ccc2c1CCO2 10.1021/acs.jmedchem.6b01194
122442293 138342 0 None -20 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138342 0 None -20 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138342 0 None -20 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
53325935 56797 0 None -436 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56797 0 None -436 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
44572172 12546 0 None -47 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12546 0 None -47 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12546 0 None -47 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
122442250 138344 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
46228438 199985 0 None -2344 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
CHEMBL595195 199985 0 None -2344 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1OC1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
134265663 163679 0 None -204 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 163679 0 None -204 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
168281505 192880 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5188678 192880 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221963 192880 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168281505 192880 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5188678 192880 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221963 192880 0 None -4 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 3 3.1 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
44572180 12562 1 None -199 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12562 1 None -199 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12562 1 None -199 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
14515725 87310 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87310 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
11291 3220 26 None -2 4 Human 7.6 pEC50 = 7.6 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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 26 None -2 4 Human 7.6 pEC50 = 7.6 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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 26 None -2 4 Human 7.6 pEC50 = 7.6 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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
71562661 87307 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 87307 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
14515725 87310 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87310 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
24773894 62980 3 None -9 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
CHEMBL178566 62980 3 None -9 2 Human 5.6 pEC50 = 5.6 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 229 0 1 1 3.2 C[C@H]1CNCCc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2004.12.080
168275195 192823 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5181991 192823 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221539 192823 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
17654 116799 95 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 COc1ccc2c(CCN)c[nH]c2c1 10.1016/j.bmcl.2014.07.062
CHEMBL337825 116799 95 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 COc1ccc2c(CCN)c[nH]c2c1 10.1016/j.bmcl.2014.07.062
11658860 2344 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
71562661 87307 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
CHEMBL2331794 87307 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 3 1 4 1.9 c1ccc(COc2noc3c2CCNCC3)cc1 10.1021/jm301656h
168275195 192823 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5181991 192823 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221539 192823 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1cccc(C2NCCc3c2[nH]c2ccc(O)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL4802359 214062 1 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
118713118 114306 2 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 206 3 2 1 2.6 CCC(N)Cc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2014.07.062
CHEMBL3330648 114306 2 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 206 3 2 1 2.6 CCC(N)Cc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2014.07.062
44572808 12706 0 None -74 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12706 0 None -74 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12706 0 None -74 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
11658860 2344 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4802359 214062 1 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
46230097 199366 0 None -15 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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 199366 0 None -15 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 217 0 2 3 0.6 O=C1NC2CCNCCN2c2ccccc21 10.1016/j.bmcl.2009.12.014
112485369 114305 2 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 222 3 2 1 3.1 CCC(N)Cc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2014.07.062
CHEMBL3330647 114305 2 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 222 3 2 1 3.1 CCC(N)Cc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2014.07.062
44412388 78185 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 78185 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
23652278 62631 17 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 62631 17 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
24773814 94859 1 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 94859 1 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
24773900 123432 8 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 123432 8 None -1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
4312735 192874 1 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192874 1 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192874 1 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
134265618 164055 0 None -204 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164055 0 None -204 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
24773894 62980 3 None -9 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
CHEMBL178566 62980 3 None -9 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
11780383 19051 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 264 1 3 2 3.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL1288870 19051 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 264 1 3 2 3.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5169776 19051 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 264 1 3 2 3.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
11780383 19051 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 264 1 3 2 3.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL1288870 19051 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 264 1 3 2 3.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5169776 19051 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 264 1 3 2 3.1 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
4312735 192874 1 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192874 1 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192874 1 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
45485751 197655 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 334 5 1 6 1.4 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Cl 10.1016/j.bmcl.2009.07.136
CHEMBL570937 197655 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 334 5 1 6 1.4 O=c1ccc(N2CCNCC2)nn1CCOc1ccccc1Cl 10.1016/j.bmcl.2009.07.136
162653458 183666 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183666 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183666 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
11658860 2344 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 51 None -17 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
162645074 183624 0 None -177 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183624 0 None -177 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183624 0 None -177 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
168272754 192794 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5179588 192794 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221399 192794 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
168272754 192794 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5179588 192794 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221399 192794 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
166 3359 18 None -36 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
3045227 3359 18 None -36 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
CHEMBL76781 3359 18 None -36 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
162653458 183666 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183666 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183666 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
10465263 64332 63 None -19 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 64332 63 None -19 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
CHEMBL4783435 214070 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL4803467 214070 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
162645074 183624 0 None -177 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183624 0 None -177 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183624 0 None -177 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4783435 214070 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL4803467 214070 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
50942111 56847 0 None -27 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56847 0 None -27 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
23652278 62631 17 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 62631 17 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
53325938 56806 0 None -32 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56806 0 None -32 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
168294447 193016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 3 3 3.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5206761 193016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 3 3 3.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222789 193016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 3 3 3.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
9794638 120789 0 None -46 2 Human 6.6 pEC50 = 6.6 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 232 2 1 2 2.8 CC1CCc2cc(F)cc3c(CCN)cn1c23 10.1016/s0960-894x(00)00141-4
CHEMBL355474 120789 0 None -46 2 Human 6.6 pEC50 = 6.6 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 232 2 1 2 2.8 CC1CCc2cc(F)cc3c(CCN)cn1c23 10.1016/s0960-894x(00)00141-4
168294447 193016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 3 3 3.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5206761 193016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 3 3 3.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222789 193016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 3 3 3.1 COc1ccccc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
166 3359 18 None -36 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
3045227 3359 18 None -36 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
CHEMBL76781 3359 18 None -36 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 226 2 1 2 2.8 C[C@@H](Cn1ccc2c1cc(Cl)c(c2)F)N 10.1021/jm301656h
50878551 90745 61 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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 90745 61 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assayAgonist activity at human 5-HT2A 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
72197485 102489 0 None 1 7 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393244 102489 0 None 1 7 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040288 102489 0 None 1 7 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
168294430 193007 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193007 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193007 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
5031728 192945 2 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5191733 192945 2 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222389 192945 2 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
168294430 193007 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193007 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193007 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
5031728 192945 2 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5191733 192945 2 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222389 192945 2 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Cl 10.1021/acsmedchemlett.1c00694
20976025 141087 46 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2014.07.062
CHEMBL382635 141087 46 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2cccc(F)c12 10.1016/j.bmcl.2014.07.062
146464681 192849 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 2 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5183463 192849 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 2 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221759 192849 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 2 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
146464681 192849 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 2 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5183463 192849 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 2 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221759 192849 0 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 2 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
168295067 193022 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5206340 193022 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222815 193022 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168295067 193022 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5206340 193022 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222815 193022 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 346 2 2 2 4.7 COc1ccc2cc(C3NCCc4c3[nH]c3ccc(F)cc43)ccc2c1 10.1021/acsmedchemlett.1c00694
168295538 193039 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207179 193039 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222923 193039 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
168295538 193039 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5207179 193039 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222923 193039 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 2 3 2 3.3 Oc1ccc2[nH]c3c(c2c1)CCNC3Cc1ccccc1 10.1021/acsmedchemlett.1c00694
145966293 164454 0 None -85 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164454 0 None -85 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
16115652 83491 0 None -26 3 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 83491 0 None -26 3 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
1355 2011 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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 88 None -4 6 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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
72197309 102498 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 318 4 1 6 0.8 CCN(CC)c1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
CHEMBL2393234 102498 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 318 4 1 6 0.8 CCN(CC)c1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
CHEMBL3040350 102498 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 318 4 1 6 0.8 CCN(CC)c1nc(N2CCN(C)CC2)nc2c1CCNCC2 10.1016/j.ejmech.2013.02.020
162643473 183615 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183615 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183615 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4764937 214069 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL4803300 214069 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
162643473 183615 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183615 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183615 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162658689 183690 0 None -47 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183690 0 None -47 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183690 0 None -47 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4764937 214069 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL4803300 214069 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
162658689 183690 0 None -47 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183690 0 None -47 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183690 0 None -47 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
118733826 120643 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3416066 120643 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3546874 120643 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 227 5 1 2 2.2 NC[C@@H]1C[C@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
53325937 56805 0 None 7 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56805 0 None 7 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
168293874 192179 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192179 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192179 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192179 0 None -3 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168273228 192799 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5178632 192799 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221423 192799 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
168273228 192799 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5178632 192799 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221423 192799 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 354 4 3 5 3.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(O)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44389646 64883 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 64883 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
74405184 186056 8 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 230 6 1 1 3.4 CCCN(CC)CCc1c[nH]c2ccccc12 10.1021/acsmedchemlett.1c00577
CHEMBL4871007 186056 8 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 230 6 1 1 3.4 CCCN(CC)CCc1c[nH]c2ccccc12 10.1021/acsmedchemlett.1c00577
168280365 191276 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5190617 191276 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
11658860 2344 51 None -17 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 51 None -17 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 51 None -17 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 51 None -17 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 51 None -17 11 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
3288856 192813 2 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5176057 192813 2 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5221496 192813 2 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 1 3.7 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1F 10.1021/acsmedchemlett.1c00694
CHEMBL4749189 214064 31 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL4802743 214064 31 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
70683433 74458 1 None -169 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A 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 74458 1 None -169 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A 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 74458 1 None -169 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A 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
11499800 89107 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89107 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89107 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
CHEMBL4749189 214064 31 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL4802743 214064 31 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
45485742 197823 0 None -30 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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 197823 0 None -30 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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
24773651 154857 0 None -5 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 154857 0 None -5 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
168292007 192988 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5200288 192988 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222607 192988 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
24773728 94860 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 94860 0 None -15 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
168292007 192988 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5200288 192988 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222607 192988 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 278 1 3 2 3.4 Cc1ccc(C2NCCc3c2[nH]c2ccc(O)cc32)cc1 10.1021/acsmedchemlett.1c00694
44225654 187190 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2A receptor expressed in mouse Swiss 3T3 cells by FLIPR assayAgonist activity at human 5HT2A receptor expressed in mouse Swiss 3T3 cells by FLIPR assay
ChEMBL 420 4 1 4 3.3 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2Cl)CC1 10.1016/j.bmcl.2009.02.071
CHEMBL492301 187190 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT2A receptor expressed in mouse Swiss 3T3 cells by FLIPR assayAgonist activity at human 5HT2A receptor expressed in mouse Swiss 3T3 cells by FLIPR assay
ChEMBL 420 4 1 4 3.3 O=S(=O)(c1ccc2c(c1)CCNCC2)N1CCC(Oc2ccccc2Cl)CC1 10.1016/j.bmcl.2009.02.071
53321948 56804 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56804 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
44404886 72225 0 None 19 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
ChEMBL 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
CHEMBL198124 72225 0 None 19 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
ChEMBL 260 6 1 3 3.3 CCCCn1cc(CCN(C)C)c2c(O)cccc21 10.1016/j.bmcl.2005.06.104
16115511 84837 0 None -72 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 84837 0 None -72 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
44572207 12702 0 None -25 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12702 0 None -25 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12702 0 None -25 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
CHEMBL4795286 214072 0 None -4 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL4803900 214072 0 None -4 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL4795286 214072 0 None -4 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL4803900 214072 0 None -4 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
168282202 192884 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192884 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192884 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192884 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192884 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192884 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
25070582 61454 28 None -316 9 Dog 5.5 pEC50 = 5.5 Functional
Agonist activity at 5HT2A receptor in dog femoral arteryAgonist activity at 5HT2A receptor in dog femoral artery
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61454 28 None -316 9 Dog 5.5 pEC50 = 5.5 Functional
Agonist activity at 5HT2A receptor in dog femoral arteryAgonist activity at 5HT2A receptor in dog femoral artery
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
168289654 192959 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5193914 192959 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5222453 192959 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
168290156 192965 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194324 192965 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222484 192965 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168289654 192959 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5193914 192959 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5222453 192959 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 270 1 3 3 3.2 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
168290156 192965 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194324 192965 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222484 192965 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 2 3.6 Fc1ncccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
10624 70300 19 None -46 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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 70300 19 None -46 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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 70300 19 None -46 3 Human 5.5 pEC50 = 5.5 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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
10332474 59655 0 None -1513 2 Human 6.5 pEC50 = 6.5 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 252 2 1 3 2.9 NCCc1cn2c3c(cc(Cl)cc13)SCC2 10.1016/s0960-894x(00)00141-4
CHEMBL172159 59655 0 None -1513 2 Human 6.5 pEC50 = 6.5 Functional
Functional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell lineFunctional agonist activity of compound was determined by fluorescence-based assay measuring intracellular calcium mobilization for 5-HT2a receptor cell line
ChEMBL 252 2 1 3 2.9 NCCc1cn2c3c(cc(Cl)cc13)SCC2 10.1016/s0960-894x(00)00141-4
44572168 12484 1 None -31 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12484 1 None -31 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12484 1 None -31 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168295285 193029 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 274 1 2 2 2.9 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5208963 193029 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 274 1 2 2 2.9 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5222859 193029 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 274 1 2 2 2.9 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
162658803 183692 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183692 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183692 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
168295285 193029 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 274 1 2 2 2.9 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5208963 193029 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 274 1 2 2 2.9 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5222859 193029 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 274 1 2 2 2.9 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
162658803 183692 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183692 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183692 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
92042921 120670 0 None -104 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3416067 120670 0 None -104 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
CHEMBL3546961 120670 0 None -104 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 227 5 1 2 2.2 NC[C@H]1C[C@@H]1c1cc(F)ccc1OCCF 10.1021/jm5019274
44572178 12561 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12561 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12561 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
122442309 138347 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138347 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138347 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
3572096 192898 1 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192898 1 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192898 1 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168274213 192810 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5178487 192810 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221472 192810 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
3572096 192898 1 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192898 1 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192898 1 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
122442309 138347 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138347 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138347 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
168274213 192810 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5178487 192810 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221472 192810 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)cc1O 10.1021/acsmedchemlett.1c00694
44316017 205452 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 205452 0 None -51 3 Human 6.4 pEC50 = 6.4 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
24826869 91102 0 None -9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 91102 0 None -9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
162652937 183662 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183662 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183662 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162652937 183662 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183662 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183662 0 None -22 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 164013 0 None -194 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164013 0 None -194 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
16115269 138129 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 138129 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
168280142 192861 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5183068 192861 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221869 192861 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
168280142 192861 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5183068 192861 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221869 192861 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 290 1 2 2 3.4 Clc1ccc2[nH]c3c(c2c1)CCNC3C1CCOCC1 10.1021/acsmedchemlett.1c00694
16115644 136960 0 None -21 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 136960 0 None -21 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
92042919 120667 0 None -89 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3416063 120667 0 None -89 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
CHEMBL3546958 120667 0 None -89 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@H]1C[C@@H]1CN 10.1021/jm5019274
44316027 205522 0 None -9 3 Human 6.4 pEC50 = 6.4 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 205522 0 None -9 3 Human 6.4 pEC50 = 6.4 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
122442263 138357 0 None -15 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138357 0 None -15 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
6092 114299 14 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 188 4 2 1 2.3 CCNCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
CHEMBL3330640 114299 14 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 188 4 2 1 2.3 CCNCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
24826788 91098 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397893 91098 0 None -17 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 236 0 1 2 1.3 O=C1c2c(Cl)cccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
162659286 183695 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183695 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183695 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162665030 183727 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4782824 183727 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803449 183727 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
168280026 192858 0 None 10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5188655 192858 0 None 10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5221857 192858 0 None 10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
4407909 192866 1 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 1 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 1 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
4407909 192866 1 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 1 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 1 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168280026 192858 0 None 10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5188655 192858 0 None 10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
CHEMBL5221857 192858 0 None 10 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 285 1 2 2 3.1 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccnc1F 10.1021/acsmedchemlett.1c00694
162665030 183727 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4782824 183727 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
CHEMBL4803449 183727 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 3.3 CCCOc1ccc2occc2c1[C@H]1C[C@@H]1CN 10.1021/acs.jmedchem.6b01194
162659286 183695 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183695 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183695 0 None -12 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
57888255 192857 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 234 1 2 1 3.4 CCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183371 192857 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 234 1 2 1 3.4 CCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221840 192857 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 234 1 2 1 3.4 CCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
57888255 192857 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 234 1 2 1 3.4 CCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183371 192857 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 234 1 2 1 3.4 CCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221840 192857 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 234 1 2 1 3.4 CCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
77379 19046 75 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2014.07.062
CHEMBL1288716 19046 75 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 194 2 2 1 2.3 NCCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2014.07.062
11291 3220 26 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
4980 3220 26 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
CHEMBL65547 3220 26 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
11291 3220 26 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
4980 3220 26 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
CHEMBL65547 3220 26 None -2 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
854024 140560 77 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2cc(F)ccc12 10.1016/j.bmcl.2014.07.062
CHEMBL381160 140560 77 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2cc(F)ccc12 10.1016/j.bmcl.2014.07.062
53317923 56846 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56846 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
44412389 78096 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 78096 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
166 3359 18 None -36 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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 18 None -36 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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 18 None -36 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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
118733774 120650 0 None -43 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120650 0 None -43 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120650 0 None -43 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
4239160 192798 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5177505 192798 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5221421 192798 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
4239160 192798 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5177505 192798 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5221421 192798 2 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 2 1 4.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
5132936 192833 1 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5181253 192833 1 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5221648 192833 1 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
5132936 192833 1 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5181253 192833 1 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5221648 192833 1 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 2 3.6 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
44626357 197552 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.136
CHEMBL570274 197552 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assay
ChEMBL 382 5 1 6 2.1 C[C@@H]1CNCCN1c1ccc(=O)n(CCOc2ccccc2C(F)(F)F)n1 10.1016/j.bmcl.2009.07.136
44412403 77798 0 None -7 3 Human 6.4 pEC50 = 6.4 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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 77798 0 None -7 3 Human 6.4 pEC50 = 6.4 Functional
Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cellsInduction of 5HT2A 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
10015414 63485 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 63485 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
107992 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
122461993 138359 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769581 138359 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771395 138359 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
107992 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
165 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
CHEMBL269521 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
DB12111 2553 49 None -6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm301656h
122461993 138359 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769581 138359 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771395 138359 0 None -3 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 271 5 1 2 3.6 C=CCOc1ccc(Cl)c(Cl)c1C1CC1CN 10.1021/acs.jmedchem.5b01153
18735305 204933 0 None -19 3 Human 6.4 pEC50 = 6.4 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 204933 0 None -19 3 Human 6.4 pEC50 = 6.4 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
122442254 138345 0 None -33 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
44572798 12650 2 None -131 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12650 2 None -131 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12650 2 None -131 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
122442254 138345 0 None -33 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122180976 121791 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 379 8 1 4 3.8 COc1cccc(CNCCc2cc(OC)c(Br)cc2OC)c1 10.1021/acs.jmedchem.2c00702
CHEMBL3589597 121791 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 379 8 1 4 3.8 COc1cccc(CNCCc2cc(OC)c(Br)cc2OC)c1 10.1021/acs.jmedchem.2c00702
26714 75791 73 None 89 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.0 Cc1cccc2c(CCN)c[nH]c12 10.1016/j.bmcl.2014.07.062
CHEMBL1522572 75791 73 None 89 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.0 Cc1cccc2c(CCN)c[nH]c12 10.1016/j.bmcl.2014.07.062
CHEMBL204839 75791 73 None 89 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.0 Cc1cccc2c(CCN)c[nH]c12 10.1016/j.bmcl.2014.07.062
46830177 8061 30 None -190 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
CHEMBL1091105 8061 30 None -190 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 378 6 2 4 3.6 COc1cc(OC2CCC(C)(C)CC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
44572812 12514 1 None -58 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12514 1 None -58 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12514 1 None -58 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
11231392 84894 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 84894 0 None -4 3 Human 6.4 pEC50 = 6.4 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
168280082 191193 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 340 7 1 6 2.6 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5189232 191193 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 340 7 1 6 2.6 COc1cc(CCNCc2cccc3c2OCO3)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
168279029 192854 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5188817 192854 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221792 192854 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
162657053 183681 0 None -38 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183681 0 None -38 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183681 0 None -38 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162657053 183681 0 None -38 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183681 0 None -38 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183681 0 None -38 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
168279029 192854 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5188817 192854 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
CHEMBL5221792 192854 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 358 1 4 3 3.6 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cc(Br)ccc1O 10.1021/acsmedchemlett.1c00694
122442254 138345 0 None -33 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138345 0 None -33 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
44572176 12560 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12560 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12560 0 None -4 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
11313985 91083 0 None -15 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 91083 0 None -15 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
CHEMBL4802921 214067 2 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Cc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
122180977 121792 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 365 7 2 4 3.5 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL3589598 121792 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 365 7 2 4 3.5 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1Br 10.1021/acs.jmedchem.2c00702
CHEMBL4802921 214067 2 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Cc1cccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
122442272 138348 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442272 138348 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
17087 114303 39 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 COc1cccc2c(CCN)c[nH]c12 10.1016/j.bmcl.2014.07.062
CHEMBL3330644 114303 39 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 COc1cccc2c(CCN)c[nH]c12 10.1016/j.bmcl.2014.07.062
77158 19047 56 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2014.07.062
CHEMBL1288717 19047 56 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 238 2 2 1 2.4 NCCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2014.07.062
156836218 188604 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 248 6 1 1 3.6 CCCN(CC)CCc1c[nH]c2ccc(F)cc12 10.1021/acsmedchemlett.1c00577
CHEMBL4877402 188604 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 248 6 1 1 3.6 CCCN(CC)CCc1c[nH]c2ccc(F)cc12 10.1021/acsmedchemlett.1c00577
CHEMBL5028990 188604 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 248 6 1 1 3.6 CCCN(CC)CCc1c[nH]c2ccc(F)cc12 10.1021/acsmedchemlett.1c00577
5 139 72 None -19 26 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
5202 139 72 None -19 26 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
CHEMBL39 139 72 None -19 26 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm801354e
DB08839 139 72 None -19 26 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
166 3359 18 None -36 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 18 None -36 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 18 None -36 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
6088 119842 56 None 100 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
CHEMBL348588 119842 56 None 100 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 10.1016/j.bmcl.2014.07.062
46884138 8443 0 None -100 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A 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 8443 0 None -100 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at 5HT2A receptorAgonist activity at 5HT2A receptor
ChEMBL 364 7 2 4 3.2 COc1cc(OCC2CCCCC2)c(F)cc1CNC(=O)[C@@H]1CCCN1 10.1016/j.bmcl.2010.01.107
10331841 169204 6 None -46 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
CHEMBL440752 169204 6 None -46 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 239 0 1 1 2.7 CC1CNCCc2ccc(Br)cc21 10.1021/jm0709034
44572810 12655 2 None -95 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12655 2 None -95 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12655 2 None -95 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
44572170 12465 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12465 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12465 1 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168291896 192985 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192985 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192985 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
CHEMBL4752798 214065 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4802821 214065 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4752798 214065 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL4802821 214065 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
10331841 169204 6 None -46 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 169204 6 None -46 3 Human 6.3 pEC50 = 6.3 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
122442270 138346 1 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
168282109 192883 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183544 192883 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221988 192883 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442270 138346 1 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
11209786 137240 0 None -36 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 137240 0 None -36 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
44572761 12680 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12680 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12680 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168282109 192883 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5183544 192883 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221988 192883 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 301 1 2 3 3.7 Cc1noc(C)c1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
53321865 56848 0 None -138 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56848 0 None -138 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
168291896 192985 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192985 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192985 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
11151653 91101 0 None -6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 91101 0 None -6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
168290300 191986 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 314 7 1 4 3.0 COc1cc(CCNCc2ccccc2F)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5201317 191986 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 314 7 1 4 3.0 COc1cc(CCNCc2ccccc2F)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
134265620 164406 0 None -426 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164406 0 None -426 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
168291130 192976 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192976 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192976 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192976 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192976 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192976 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
157292621 192971 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5199923 192971 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222513 192971 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
157292621 192971 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5199923 192971 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222513 192971 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 2 3 2.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
44573014 12521 1 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12521 1 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12521 1 None -13 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
14515725 87310 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87310 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
14515725 87310 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
CHEMBL2331807 87310 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 244 2 1 4 1.2 O=c1c2c(on1Cc1ccccc1)CCNCC2 10.1021/jm301656h
16115271 79108 0 None -5 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 79108 0 None -5 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
4543677 192790 1 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192790 1 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192790 1 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192790 1 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192790 1 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192790 1 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168268706 192757 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5170614 192757 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221142 192757 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
46228430 199738 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 199738 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
44573018 12644 1 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12644 1 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12644 1 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168268706 192757 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5170614 192757 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221142 192757 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 282 1 3 2 3.2 Oc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1 10.1021/acsmedchemlett.1c00694
162676555 183789 0 None -22 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4800666 183789 0 None -22 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4804119 183789 0 None -22 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
44572802 12444 2 None -123 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12444 2 None -123 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12444 2 None -123 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
53324629 56799 0 None 4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56799 0 None 4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
162676555 183789 0 None -22 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4800666 183789 0 None -22 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
CHEMBL4804119 183789 0 None -22 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
168275014 192820 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177386 192820 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221524 192820 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
15760 113079 57 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.0 Cc1ccc2[nH]cc(CCN)c2c1 10.1016/j.bmcl.2014.07.062
CHEMBL331241 113079 57 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.0 Cc1ccc2[nH]cc(CCN)c2c1 10.1016/j.bmcl.2014.07.062
72197484 102494 0 None 1 9 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 102494 0 None 1 9 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 102494 0 None 1 9 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
12833 67661 17 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 208 2 2 1 2.7 CC(N)Cc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2014.07.062
CHEMBL1906905 67661 17 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 208 2 2 1 2.7 CC(N)Cc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2014.07.062
72197486 102503 0 None 1 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 102503 0 None 1 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 102503 0 None 1 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
11291 3220 26 None -2 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.2c00129
4980 3220 26 None -2 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.2c00129
CHEMBL65547 3220 26 None -2 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.2c00129
11291 3220 26 None -2 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00577
4980 3220 26 None -2 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00577
CHEMBL65547 3220 26 None -2 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assayAgonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.1c00577
152743520 189979 1 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 326 8 1 5 2.9 COc1cc(CCNCc2ccccc2OC)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5170895 189979 1 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 326 8 1 5 2.9 COc1cc(CCNCc2ccccc2OC)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
18735313 204934 1 None -93 3 Human 6.2 pEC50 = 6.2 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 204934 1 None -93 3 Human 6.2 pEC50 = 6.2 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
168275014 192820 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177386 192820 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221524 192820 0 None -3 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 218 1 2 1 2.9 CCC1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
11493484 89070 0 None -141 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89070 0 None -141 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89070 0 None -141 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
11666237 89112 0 None -35 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89112 0 None -35 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89112 0 None -35 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
10064386 63317 4 None -30 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 63317 4 None -30 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
44572806 12654 1 None -38 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12654 1 None -38 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12654 1 None -38 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
11658860 2344 51 None -17 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 51 None -17 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
146025684 183635 0 None -14 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183635 0 None -14 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183635 0 None -14 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
9859257 205123 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 205123 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
11695000 89071 0 None -17 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89071 0 None -17 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89071 0 None -17 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
53323196 56849 0 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56849 0 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
11777150 62605 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 62605 0 None -20 3 Human 7.2 pEC50 = 7.2 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
1355 2011 88 None -4 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 88 None -4 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 88 None -4 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 88 None -4 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm0709034
10036629 64637 0 None -7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 64637 0 None -7 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
9990808 122772 0 None -10 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 122772 0 None -10 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
11949710 199902 0 None -67 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 199902 0 None -67 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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
146025684 183635 0 None -14 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183635 0 None -14 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183635 0 None -14 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
168276822 190123 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 324 6 1 5 2.8 COc1cc(CCNC2COc3ccccc32)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5173321 190123 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 324 6 1 5 2.8 COc1cc(CCNC2COc3ccccc32)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
44404883 72062 32 None -21 3 Human 6.2 pEC50 = 6.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
CHEMBL197664 72062 32 None -21 3 Human 6.2 pEC50 = 6.2 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay
ChEMBL 218 3 1 3 2.0 CN(C)CCc1cn(C)c2cccc(O)c12 10.1016/j.bmcl.2005.06.104
24826790 91094 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
CHEMBL2397889 91094 0 None -12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 216 0 1 2 1.0 Cc1cccc2c1C(=O)N1CCNC[C@H]1C2 10.1016/j.bmcl.2013.04.061
57888169 192907 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5194866 192907 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222124 192907 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
57888169 192907 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5194866 192907 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222124 192907 0 None -4 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.6 Clc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
143111395 192815 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 248 2 2 1 3.8 CCCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177927 192815 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 248 2 2 1 3.8 CCCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221502 192815 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 248 2 2 1 3.8 CCCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442300 138349 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138349 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138349 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
143111395 192815 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 248 2 2 1 3.8 CCCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177927 192815 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 248 2 2 1 3.8 CCCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221502 192815 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 248 2 2 1 3.8 CCCC1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
53324630 56803 0 None -128 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56803 0 None -128 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
45485725 197827 0 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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 197827 0 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells assessed as induction of calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A 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 138349 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138349 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138349 0 None -4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
44572751 12499 1 None -87 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12499 1 None -87 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12499 1 None -87 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
122442286 138351 0 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
25070582 61454 28 None -6 9 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61454 28 None -6 9 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
122442286 138351 0 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138351 0 None -13 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
72197311 102491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 348 2 1 7 0.5 CN1CCN(c2nc3c(c(N4CCSCC4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL2393236 102491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 348 2 1 7 0.5 CN1CCN(c2nc3c(c(N4CCSCC4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
CHEMBL3040299 102491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 348 2 1 7 0.5 CN1CCN(c2nc3c(c(N4CCSCC4)n2)CCNCC3)CC1 10.1016/j.ejmech.2013.02.020
118733820 120666 0 None -4 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3416062 120666 0 None -4 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL3546957 120666 0 None -4 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 221 5 1 2 2.5 C=CCOc1ccc(F)cc1[C@@H]1C[C@H]1CN 10.1021/jm5019274
CHEMBL5078999 214598 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL None None None COc1ccc2[nH]cc(CCN3CCC3)c2c1 10.1021/acsmedchemlett.2c00129
1355 2011 88 None -4 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2013.02.020
142 2011 88 None -4 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2013.02.020
CHEMBL478 2011 88 None -4 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2013.02.020
DB12110 2011 88 None -4 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAgonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2013.02.020
1150 3878 121 None 41 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1016/j.bmcl.2014.07.062
125 3878 121 None 41 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1016/j.bmcl.2014.07.062
CHEMBL6640 3878 121 None 41 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1016/j.bmcl.2014.07.062
DB08653 3878 121 None 41 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1016/j.bmcl.2014.07.062
5 139 72 None -19 26 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
5202 139 72 None -19 26 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
CHEMBL39 139 72 None -19 26 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/ml200206z
DB08839 139 72 None -19 26 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A 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
46228437 199984 1 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 199984 1 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 343 3 1 4 3.6 Clc1ccccc1O[C@H]1CCCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
5 139 72 None -19 26 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
5202 139 72 None -19 26 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
CHEMBL39 139 72 None -19 26 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2007.10.100
DB08839 139 72 None -19 26 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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
46230098 199329 0 None -34 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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 199329 0 None -34 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A 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
24826786 91086 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
CHEMBL2397881 91086 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 202 0 1 2 0.7 O=C1c2ccccc2C[C@@H]2CNCCN12 10.1016/j.bmcl.2013.04.061
168 3982 15 None -66 5 Human 6.1 pEC50 = 6.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 15 None -66 5 Human 6.1 pEC50 = 6.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 15 None -66 5 Human 6.1 pEC50 = 6.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
168291564 192983 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192983 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192983 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
9990808 122772 0 None -10 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 122772 0 None -10 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
168291564 192983 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192983 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192983 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
4305260 191025 1 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5186877 191025 1 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
4305260 191025 1 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
CHEMBL5186877 191025 1 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 288 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cccs1 10.1021/acsmedchemlett.1c00694
44572174 12547 0 None -208 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12547 0 None -208 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12547 0 None -208 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168286640 192928 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192928 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192928 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168286640 192928 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192928 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192928 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
162652983 183663 0 None -37 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183663 0 None -37 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183663 0 None -37 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162652983 183663 0 None -37 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183663 0 None -37 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183663 0 None -37 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
1355 2011 88 None -4 6 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
142 2011 88 None -4 6 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
CHEMBL478 2011 88 None -4 6 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
DB12110 2011 88 None -4 6 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.bmcl.2003.05.001
190006 114301 24 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.0 Cc1ccc2c(CCN)c[nH]c2c1 10.1016/j.bmcl.2014.07.062
CHEMBL3330642 114301 24 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 174 2 2 1 2.0 Cc1ccc2c(CCN)c[nH]c2c1 10.1016/j.bmcl.2014.07.062
9901086 187631 33 None -95 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 187631 33 None -95 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
162658153 183685 0 None -28 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183685 0 None -28 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183685 0 None -28 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183685 0 None -28 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183685 0 None -28 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183685 0 None -28 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
9901086 187631 33 None -95 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
CHEMBL494947 187631 33 None -95 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.1021/jm301656h
11264955 204961 0 None -18 3 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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 204961 0 None -18 3 Human 7.1 pEC50 = 7.1 Functional
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate readerFunctional activity against human 5-hydroxytryptamine 2A 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
53317925 56852 0 None -91 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56852 0 None -91 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
122442251 138360 0 None -47 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
72197668 102495 0 None -4 7 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393246 102495 0 None -4 7 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040325 102495 0 None -4 7 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
44572164 12683 0 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12683 0 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12683 0 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168291006 192975 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5199780 192975 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5222544 192975 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
168291006 192975 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5199780 192975 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5222544 192975 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 380 1 2 2 5.2 Cc1cc(C2NCCc3c2[nH]c2ccc(Cl)cc32)sc1Br 10.1021/acsmedchemlett.1c00694
122442251 138360 0 None -47 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138360 0 None -47 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
53325936 56802 0 None -436 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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 56802 0 None -436 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in CHOK1 cells assessed as induction of intracellular calcium release by FLIPR assayAgonist activity at human recombinant 5HT2A 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
16115381 83443 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 83443 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
168277089 192839 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 3 4 1.8 Cn1ccnc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5179053 192839 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 3 4 1.8 Cn1ccnc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221673 192839 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 3 4 1.8 Cn1ccnc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
168277089 192839 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 3 4 1.8 Cn1ccnc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5179053 192839 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 3 4 1.8 Cn1ccnc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221673 192839 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 268 1 3 4 1.8 Cn1ccnc1C1NCCc2c1[nH]c1ccc(O)cc21 10.1021/acsmedchemlett.1c00694
20026449 87306 1 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331793 87306 1 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
11264345 130399 5 None -38 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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 130399 5 None -38 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulationAgonist activity at human 5HT2A 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
122442275 138361 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138361 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138361 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
20026449 87306 1 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
CHEMBL2331793 87306 1 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
ChEMBL 182 2 1 4 0.8 CCOc1noc2c1CCNCC2 10.1021/jm301656h
3549735 192207 2 None -6 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5204651 192207 2 None -6 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
122442275 138361 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138361 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138361 0 None -9 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
168268877 189970 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 189970 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
14107683 178126 22 None 2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
CHEMBL4648350 178126 22 None 2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
168268877 189970 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 189970 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
14107683 178126 22 None 2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
CHEMBL4648350 178126 22 None 2 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acs.jnatprod.9b01061
12834 207926 26 None 18 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 192 2 2 1 2.2 CC(N)Cc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2014.07.062
CHEMBL96816 207926 26 None 18 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 192 2 2 1 2.2 CC(N)Cc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2014.07.062
90489020 190873 9 None 14 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2ccccc2O)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5184791 190873 9 None 14 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2ccccc2O)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
9881885 64109 0 None -15 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 64109 0 None -15 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
44389645 64181 0 None -26 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 64181 0 None -26 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
10036629 64637 0 None -7 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 64637 0 None -7 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
146464686 191997 0 None 8 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5201492 191997 0 None 8 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
3549735 192207 2 None -6 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5204651 192207 2 None -6 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 300 1 2 1 4.2 Fc1ccccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
3356430 193046 2 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193046 2 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193046 2 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
122442250 138344 0 None -12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442270 138346 1 None -20 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
3356430 193046 2 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193046 2 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193046 2 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
122442250 138344 0 None -12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138344 0 None -12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442270 138346 1 None -20 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138346 1 None -20 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
168277801 192844 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5176879 192844 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221724 192844 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
168294156 193005 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
146464686 191997 0 None 8 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5201492 191997 0 None 8 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 3 4 1.9 Oc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
168277801 192844 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5176879 192844 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5221724 192844 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 3 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3CCc1ccccc1 10.1021/acsmedchemlett.1c00694
168294156 193005 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 0 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
122442272 138348 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442272 138348 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138348 0 None -19 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
122442260 138354 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
168280365 191276 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
CHEMBL5190617 191276 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayAgonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay
ChEMBL 312 7 2 5 2.6 COc1cc(CCNCc2cccc(O)c2)c(OC)cc1C#N 10.1021/acs.jmedchem.2c00702
11264345 130399 5 None -38 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1016/j.bmcl.2004.12.080
CHEMBL368016 130399 5 None -38 3 Human 6.1 pEC50 = 6.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
ChEMBL 213 0 1 1 2.7 CC1CNCCc2ccc(Cl)c(F)c21 10.1016/j.bmcl.2004.12.080
168295069 193027 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5208635 193027 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222843 193027 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
122442260 138354 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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 138354 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A 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
168295069 193027 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5208635 193027 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
CHEMBL5222843 193027 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 317 1 2 2 4.1 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccncc1Cl 10.1021/acsmedchemlett.1c00694
11579853 89085 0 None -70 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2337504 89085 0 None -70 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
CHEMBL2365200 89085 0 None -70 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assay
ChEMBL 230 1 2 2 1.4 CCc1cc(C)c2c(c1)[C@H]1CNC[C@@H]1NC2=O 10.1016/j.bmcl.2012.10.091
11448649 83433 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 83433 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
11949712 202161 0 None -870 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A 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 202161 0 None -870 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human 5HT2A receptor by FLIPR assayAgonist activity against human 5HT2A receptor by FLIPR assay
ChEMBL 329 3 1 4 3.2 Clc1ccccc1O[C@H]1CCc2ccc(N3CCNCC3)nc21 10.1016/j.bmcl.2009.10.112
11300712 141686 0 None -72 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 141686 0 None -72 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
168271458 190608 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5180800 190608 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
11652452 89126 0 None -26 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89126 0 None -26 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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 89126 0 None -26 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at 5-HT2A receptor in HEK293E cells assessed as elevation of intracellular calcium level measured for 90 secs by FLIPR assayAgonist activity at 5-HT2A 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
168271458 190608 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
CHEMBL5180800 190608 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 266 1 2 1 3.5 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1 10.1021/acsmedchemlett.1c00694
168284944 192913 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5192557 192913 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222162 192913 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
46937339 74209 0 None -42 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A 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 74209 0 None -42 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assayAgonist activity at human 5HT2A 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
168284944 192913 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5192557 192913 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
CHEMBL5222162 192913 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 284 1 2 3 2.8 Clc1ccc2[nH]c3c(c2c1)CCNC3c1cncnc1 10.1021/acsmedchemlett.1c00694
19219 119245 30 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 COc1cccc2[nH]cc(CCN)c12 10.1016/j.bmcl.2014.07.062
CHEMBL343529 119245 30 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assayAgonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
ChEMBL 190 3 2 2 1.7 COc1cccc2[nH]cc(CCN)c12 10.1016/j.bmcl.2014.07.062
11291 3220 26 None -1 4 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
4980 3220 26 None -1 4 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
CHEMBL65547 3220 26 None -1 4 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
11291 3220 26 None -1 4 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
4980 3220 26 None -1 4 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
CHEMBL65547 3220 26 None -1 4 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assayAgonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acs.jnatprod.9b01061
17954204 63938 23 None -7 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 63938 23 None -7 3 Human 7.1 pEC50 = 7.1 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
CHEMBL5094489 215497 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL None None None c1ccc2c(CCN3CCC3)c[nH]c2c1 10.1021/acsmedchemlett.2c00129
118733802 120653 0 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120653 0 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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 120653 0 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5-HT2A 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
16115267 84793 0 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 84793 0 None -5 3 Human 7.0 pEC50 = 7.0 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
44572166 12460 0 None -30 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12460 0 None -30 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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 12460 0 None -30 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A 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
168276733 192831 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5180401 192831 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
CHEMBL5221642 192831 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 272 1 2 1 4.1 Fc1ccc2[nH]c3c(c2c1)CCNC3C1CCCCC1 10.1021/acsmedchemlett.1c00694
4995534 192852 1 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5188386 192852 1 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221773 192852 1 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
4995534 192852 1 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5188386 192852 1 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
CHEMBL5221773 192852 1 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 366 1 2 2 4.9 Clc1ccc2[nH]c3c(c2c1)CCNC3c1ccc(Br)s1 10.1021/acsmedchemlett.1c00694
122442307 138355 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3770950 138355 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771391 138355 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
71682217 91118 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 91118 0 None -11 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
230 4119 25 None -93 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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 25 None -93 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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 25 None -93 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysisAgonist activity at human cloned 5HT2A receptor expressed in CHO 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
CHEMBL4742882 214063 2 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL4802403 214063 2 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
122442307 138355 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3770950 138355 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL3771391 138355 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1cc(Cl)c(Cl)cc1OCCF 10.1021/acs.jmedchem.5b01153
CHEMBL4742882 214063 2 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
CHEMBL4802403 214063 2 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL None None None Oc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1021/acsmedchemlett.1c00694
162650400 183649 0 None -346 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183649 0 None -346 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183649 0 None -346 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162668367 183739 0 None -43 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183739 0 None -43 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183739 0 None -43 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
122442281 138352 0 None -5 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770058 138352 0 None -5 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771388 138352 0 None -5 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
122442281 138352 0 None -5 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3770058 138352 0 None -5 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
CHEMBL3771388 138352 0 None -5 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 261 5 1 2 2.9 NCC1CC1c1c(OCCF)ccc(Cl)c1F 10.1021/acs.jmedchem.5b01153
162668367 183739 0 None -43 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183739 0 None -43 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183739 0 None -43 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162650400 183649 0 None -346 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183649 0 None -346 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183649 0 None -346 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
16047544 12648 8 None -72 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL1187185 12648 8 None -72 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
CHEMBL492916 12648 8 None -72 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAgonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 225 2 1 1 2.5 NCC1CC1c1ccccc1Br 10.1021/jm801354e
24773900 123432 8 None -1 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 123432 8 None -1 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
122442310 138358 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770011 138358 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771394 138358 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
11492162 72053 3 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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 72053 3 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assayEffective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A 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
46230100 199319 0 None -38 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
CHEMBL590531 199319 0 None -38 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assayAgonist activity at human recombinant 5HT2A receptor expressed in HEK293E cells by FLIPR assay
ChEMBL 231 0 2 3 0.9 Cc1ccc2c(c1)N1CCNCCC1NC2=O 10.1016/j.bmcl.2009.12.014
122442310 138358 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3770011 138358 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
CHEMBL3771394 138358 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assayAgonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL 277 5 1 2 3.4 NCC1CC1c1c(OCCF)ccc(Cl)c1Cl 10.1021/acs.jmedchem.5b01153
72197483 102502 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 340 3 1 5 2.3 c1ccc(Cc2nc3c(c(N4CCSCC4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393242 102502 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 340 3 1 5 2.3 c1ccc(Cc2nc3c(c(N4CCSCC4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040360 102502 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assayAntagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
ChEMBL 340 3 1 5 2.3 c1ccc(Cc2nc3c(c(N4CCSCC4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
24826868 91082 1 None -10 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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 91082 1 None -10 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5-HT2A receptor expressed in HEK293E cells assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human 5-HT2A 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
10017556 161878 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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 161878 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol releaseEffective concentration towards 5-hydroxytryptamine 2A 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
4363390 192870 2 None 21 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5184885 192870 2 None 21 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5221904 192870 2 None 21 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
162669436 183745 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183745 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183745 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
162669436 183745 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183745 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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 183745 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assayAgonist activity at human 5-HT2A receptor expressed in 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
4363390 192870 2 None 21 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5184885 192870 2 None 21 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
CHEMBL5221904 192870 2 None 21 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 344 1 2 1 4.3 Fc1ccc2[nH]c3c(c2c1)CCNC3c1ccccc1Br 10.1021/acsmedchemlett.1c00694
134265732 163807 0 None -776 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 163807 0 None -776 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
134265675 164367 0 None -13 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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 164367 0 None -13 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant 5-HT2A receptor (unknown origin) expressed in HEK293 cells assessed as increase in [3H]-inositol phosphate accumulation by scintillation counting methodAgonist activity at recombinant 5-HT2A 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
44420682 137608 0 None -3 3 Human 6.0 pEC50 = 6 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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 137608 0 None -3 3 Human 6.0 pEC50 = 6 Functional
Activity at human 5HT2A expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assayActivity at human 5HT2A 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
11750471 201117 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 418 4 2 4 4.6 COc1ccc(NC(=O)Nc2ccc(F)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL603078 201117 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 418 4 2 4 4.6 COc1ccc(NC(=O)Nc2ccc(F)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
175 3655 44 None - 1 Human 9.5 pIC50 = 9.5 Functional
Compound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptorCompound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptor
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/s0960-894x(00)00483-2
68186 3655 44 None - 1 Human 9.5 pIC50 = 9.5 Functional
Compound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptorCompound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptor
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/s0960-894x(00)00483-2
CHEMBL79834 3655 44 None - 1 Human 9.5 pIC50 = 9.5 Functional
Compound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptorCompound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptor
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/s0960-894x(00)00483-2
156014242 177187 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 647 11 2 7 5.5 CN1CCC(N(Cc2ccc(F)cc2)C(=O)NCc2ccc(OCC(O)CN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1021/acs.jmedchem.0c00002
CHEMBL4635010 177187 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 647 11 2 7 5.5 CN1CCC(N(Cc2ccc(F)cc2)C(=O)NCc2ccc(OCC(O)CN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1021/acs.jmedchem.0c00002
11684204 200598 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 468 4 2 4 5.5 COc1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL599226 200598 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 468 4 2 4 5.5 COc1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11453346 201091 1 None - 1 Human 9.4 pIC50 = 9.4 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2cccc(Cl)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL602874 201091 1 None - 1 Human 9.4 pIC50 = 9.4 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2cccc(Cl)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11774776 201215 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 430 5 2 5 4.5 COc1ccc(NC(=O)Nc2ccc(OC)c(-c3c(Br)cnn3C)c2)cc1 10.1021/jm9007328
CHEMBL603609 201215 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 430 5 2 5 4.5 COc1ccc(NC(=O)Nc2ccc(OC)c(-c3c(Br)cnn3C)c2)cc1 10.1021/jm9007328
11294575 200597 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 478 4 2 4 5.3 COc1ccc(NC(=O)Nc2ccc(Br)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL599225 200597 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 478 4 2 4 5.3 COc1ccc(NC(=O)Nc2ccc(Br)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11625339 201111 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 392 4 2 4 4.7 COc1ccc(NC(=O)Nc2ccc(F)c(F)c2)cc1-c1c(Cl)cnn1C 10.1021/jm9007328
CHEMBL603061 201111 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 392 4 2 4 4.7 COc1ccc(NC(=O)Nc2ccc(F)c(F)c2)cc1-c1c(Cl)cnn1C 10.1021/jm9007328
11429246 202291 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 390 4 2 4 5.0 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Cl)cnn1C 10.1021/jm9007328
CHEMBL610208 202291 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 390 4 2 4 5.0 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Cl)cnn1C 10.1021/jm9007328
168286940 192281 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 454 7 1 4 4.0 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5205903 192281 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 454 7 1 4 4.0 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
145993172 166996 0 None 1 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 423 6 0 5 3.8 O=C1C2CC=CCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4287980 166996 0 None 1 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 423 6 0 5 3.8 O=C1C2CC=CCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
25207724 178279 21 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 413 8 2 3 4.3 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCNCC2)cc1 10.1021/acs.jmedchem.0c00002
CHEMBL4644559 178279 21 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 413 8 2 3 4.3 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCNCC2)cc1 10.1021/acs.jmedchem.0c00002
CHEMBL4650860 178279 21 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 413 8 2 3 4.3 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCNCC2)cc1 10.1021/acs.jmedchem.0c00002
11683556 200420 58 None - 1 Human 9.2 pIC50 = 9.2 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 436 4 2 4 4.8 COc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL598172 200420 58 None - 1 Human 9.2 pIC50 = 9.2 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 436 4 2 4 4.8 COc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1-c1c(Br)cnn1C 10.1021/jm9007328
2389 3331 118 None -1 29 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
5073 3331 118 None -1 29 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
96 3331 118 None -1 29 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
CHEMBL85 3331 118 None -1 29 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
DB00734 3331 118 None -1 29 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
2389 3331 118 None -1 29 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
5073 3331 118 None -1 29 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
96 3331 118 None -1 29 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
CHEMBL85 3331 118 None -1 29 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
DB00734 3331 118 None -1 29 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assayAntagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2019.07.050
11247569 199420 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL591223 199420 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 434 4 2 4 5.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11567937 200982 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 418 4 2 4 4.6 COc1ccc(NC(=O)Nc2cccc(F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL602064 200982 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 418 4 2 4 4.6 COc1ccc(NC(=O)Nc2cccc(F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11519011 201090 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 502 4 2 4 6.2 COc1ccc(NC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL602873 201090 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 502 4 2 4 6.2 COc1ccc(NC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
10595416 177383 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 371 7 0 4 4.0 COc1cccc(C(=O)C2CCN(CCc3ccc(F)cc3)CC2)c1OC 10.1021/acs.jmedchem.0c01058
CHEMBL4638006 177383 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 371 7 0 4 4.0 COc1cccc(C(=O)C2CCN(CCc3ccc(F)cc3)CC2)c1OC 10.1021/acs.jmedchem.0c01058
10595416 177383 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 371 7 0 4 4.0 COc1cccc(C(=O)C2CCN(CCc3ccc(F)cc3)CC2)c1OC 10.1021/acs.jmedchem.0c01058
CHEMBL4638006 177383 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 371 7 0 4 4.0 COc1cccc(C(=O)C2CCN(CCc3ccc(F)cc3)CC2)c1OC 10.1021/acs.jmedchem.0c01058
156020283 178084 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 646 11 2 8 4.8 CN1CCC(N(Cc2ccc(F)cc2)C(=O)NCc2ccc(OCC(O)CN3CCN(c4nsc5ccccc45)CC3)cc2)CC1 10.1021/acs.jmedchem.0c00002
CHEMBL4647697 178084 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 646 11 2 8 4.8 CN1CCC(N(Cc2ccc(F)cc2)C(=O)NCc2ccc(OCC(O)CN3CCN(c4nsc5ccccc45)CC3)cc2)CC1 10.1021/acs.jmedchem.0c00002
11675550 200421 0 None - 1 Human 9.0 pIC50 = 9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 392 4 2 4 4.7 COc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1-c1c(Cl)cnn1C 10.1021/jm9007328
CHEMBL598173 200421 0 None - 1 Human 9.0 pIC50 = 9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 392 4 2 4 4.7 COc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1-c1c(Cl)cnn1C 10.1021/jm9007328
11710154 201464 0 None - 1 Human 9.0 pIC50 = 9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 356 4 2 4 4.4 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1ccnn1C 10.1021/jm9007328
CHEMBL605001 201464 0 None - 1 Human 9.0 pIC50 = 9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 356 4 2 4 4.4 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1ccnn1C 10.1021/jm9007328
11719283 201744 0 None - 1 Human 9.0 pIC50 = 9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 446 5 2 4 5.7 COc1ccc(NC(=O)Nc2ccc(F)cc2)cc1-c1c(Br)cnn1C(C)C 10.1021/jm9007328
CHEMBL606622 201744 0 None - 1 Human 9.0 pIC50 = 9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 446 5 2 4 5.7 COc1ccc(NC(=O)Nc2ccc(F)cc2)cc1-c1c(Br)cnn1C(C)C 10.1021/jm9007328
145988497 167191 0 None 7 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 411 6 0 5 3.6 O=C1C2CCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4291387 167191 0 None 7 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 411 6 0 5 3.6 O=C1C2CCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
129186554 157818 0 None 2 6 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 408 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4083333 157818 0 None 2 6 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 408 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
11154832 200419 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 436 4 2 4 4.8 COc1ccc(NC(=O)Nc2cc(F)cc(F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL598171 200419 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 436 4 2 4 4.8 COc1ccc(NC(=O)Nc2cc(F)cc(F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11719622 201387 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 462 5 2 4 6.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C(C)C 10.1021/jm9007328
CHEMBL604586 201387 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 462 5 2 4 6.2 COc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C(C)C 10.1021/jm9007328
11431347 201672 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 468 4 2 4 5.8 COc1ccc(NC(=O)Nc2ccc(Cl)cc2Cl)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL606178 201672 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 468 4 2 4 5.8 COc1ccc(NC(=O)Nc2ccc(Cl)cc2Cl)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11166827 200588 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 448 5 2 4 5.5 CCOc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL599193 200588 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 448 5 2 4 5.5 CCOc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11328744 200589 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 462 5 2 4 5.9 CC(C)Oc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL599194 200589 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 462 5 2 4 5.9 CC(C)Oc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
11531833 200844 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 418 4 2 4 4.6 COc1ccc(NC(=O)Nc2ccccc2F)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL601097 200844 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 418 4 2 4 4.6 COc1ccc(NC(=O)Nc2ccccc2F)cc1-c1c(Br)cnn1C 10.1021/jm9007328
135507495 201587 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 420 3 3 4 4.9 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1O 10.1021/jm9007328
CHEMBL605636 201587 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 420 3 3 4 4.9 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1O 10.1021/jm9007328
11374796 201675 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 468 4 2 4 5.5 COc1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL606191 201675 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 468 4 2 4 5.5 COc1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
162646896 179572 0 None -3 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR methodAntagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR method
ChEMBL 421 6 0 5 4.2 O=C1COc2ccccc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
CHEMBL4741908 179572 0 None -3 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR methodAntagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR method
ChEMBL 421 6 0 5 4.2 O=C1COc2ccccc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
11627746 197400 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Agonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulationAgonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 517 7 2 5 5.6 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2009.07.073
CHEMBL569475 197400 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Agonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulationAgonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 517 7 2 5 5.6 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2009.07.073
164143991 190154 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 432 9 1 4 3.8 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCCCF)cc2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5173703 190154 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 432 9 1 4 3.8 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCCCF)cc2)CC1 10.1016/j.ejmech.2022.114246
156011636 177421 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 613 10 2 7 3.9 CN1CCC(N(Cc2ccc(F)cc2)C(=O)NCc2ccc(OCC(O)CN3CCN(C(=O)OC(C)(C)C)CC3)cc2)CC1 10.1021/acs.jmedchem.0c00002
CHEMBL4638548 177421 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 613 10 2 7 3.9 CN1CCC(N(Cc2ccc(F)cc2)C(=O)NCc2ccc(OCC(O)CN3CCN(C(=O)OC(C)(C)C)CC3)cc2)CC1 10.1021/acs.jmedchem.0c00002
168282398 191205 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 482 9 1 4 4.7 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCCCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5189473 191205 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 482 9 1 4 4.7 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCCCC(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
11656729 200685 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 536 4 2 4 6.5 COc1ccc(NC(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
CHEMBL599828 200685 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 536 4 2 4 6.5 COc1ccc(NC(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cc1-c1c(Br)cnn1C 10.1021/jm9007328
44608359 157344 39 None -1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 424 4 0 7 3.2 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2=O 10.1016/j.bmc.2017.07.040
CHEMBL4077702 157344 39 None -1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 424 4 0 7 3.2 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2=O 10.1016/j.bmc.2017.07.040
168276428 190116 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 490 7 1 4 4.6 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OC(F)(F)C(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5173149 190116 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 490 7 1 4 4.6 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OC(F)(F)C(F)(F)F)cc2)CC1 10.1016/j.ejmech.2022.114246
129186534 159696 0 None -3 6 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 426 4 0 6 3.9 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2F 10.1016/j.bmc.2017.07.040
CHEMBL4104261 159696 0 None -3 6 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 426 4 0 6 3.9 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2F 10.1016/j.bmc.2017.07.040
145991244 166802 0 None -1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 411 6 0 5 3.4 CC1(C)C2C(=O)N(CCCCN3CCN(c4cccc5sccc45)CC3)C(=O)C21 10.1016/j.ejmech.2017.12.099
CHEMBL4284353 166802 0 None -1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 411 6 0 5 3.4 CC1(C)C2C(=O)N(CCCCN3CCN(c4cccc5sccc45)CC3)C(=O)C21 10.1016/j.ejmech.2017.12.099
22733860 186878 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 357 6 1 4 3.7 COc1c(O)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
CHEMBL489624 186878 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 357 6 1 4 3.7 COc1c(O)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
135398745 2914 112 None -1 33 Human 7.0 pIC50 = 7 Functional
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2015.07.030
47 2914 112 None -1 33 Human 7.0 pIC50 = 7 Functional
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2015.07.030
CHEMBL715 2914 112 None -1 33 Human 7.0 pIC50 = 7 Functional
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2015.07.030
DB00334 2914 112 None -1 33 Human 7.0 pIC50 = 7 Functional
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2015.07.030
168286241 191561 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 441 9 1 3 5.1 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCC(N(C)C)C2)cc1 10.1016/j.ejmech.2022.114246
CHEMBL5194786 191561 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 441 9 1 3 5.1 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCC(N(C)C)C2)cc1 10.1016/j.ejmech.2022.114246
24861189 199973 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 328 6 2 3 3.2 CCNCCc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12 10.1016/j.bmc.2009.09.023
CHEMBL595133 199973 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 328 6 2 3 3.2 CCNCCc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12 10.1016/j.bmc.2009.09.023
145993577 167386 0 None -85 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 453 6 0 5 4.9 O=C1CC2(CCCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4295055 167386 0 None -85 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 453 6 0 5 4.9 O=C1CC2(CCCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
156017859 177889 0 None -5 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 432 6 0 8 3.2 N#Cc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
CHEMBL4644742 177889 0 None -5 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 432 6 0 8 3.2 N#Cc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
127050764 140261 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 435 8 1 4 4.9 CC(=O)Nc1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805600 140261 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 435 8 1 4 4.9 CC(=O)Nc1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
145976732 163510 0 None -9 3 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4202443 163510 0 None -9 3 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
156021344 178169 0 None -691 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sc(F)cc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4649106 178169 0 None -691 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sc(F)cc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
24861190 201668 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 342 7 2 3 3.5 CCCNCCc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12 10.1016/j.bmc.2009.09.023
CHEMBL606150 201668 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 342 7 2 3 3.5 CCCNCCc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12 10.1016/j.bmc.2009.09.023
1524 2181 96 None 1 18 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2014.12.045
197 2181 96 None 1 18 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2014.12.045
3822 2181 96 None 1 18 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2014.12.045
88 2181 96 None 1 18 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2014.12.045
CHEMBL51 2181 96 None 1 18 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2014.12.045
DB12465 2181 96 None 1 18 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/j.ejmech.2014.12.045
156018685 177867 0 None -2 6 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 432 6 0 8 3.2 N#Cc1ccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n2c1 10.1016/j.bmcl.2020.127027
CHEMBL4644391 177867 0 None -2 6 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 432 6 0 8 3.2 N#Cc1ccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n2c1 10.1016/j.bmcl.2020.127027
22733860 186878 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 357 6 1 4 3.7 COc1c(O)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
CHEMBL489624 186878 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 357 6 1 4 3.7 COc1c(O)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
129186544 161074 0 None -3 6 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
CHEMBL4087132 161074 0 None -3 6 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
CHEMBL4116744 161074 0 None -3 6 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
168286241 191561 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 441 9 1 3 5.1 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCC(N(C)C)C2)cc1 10.1016/j.ejmech.2022.114246
CHEMBL5194786 191561 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 441 9 1 3 5.1 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCC(N(C)C)C2)cc1 10.1016/j.ejmech.2022.114246
242 470 124 None -229 33 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
34 470 124 None -229 33 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
60795 470 124 None -229 33 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
CHEMBL1112 470 124 None -229 33 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
DB01238 470 124 None -229 33 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
127050765 140214 0 None -45 3 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805077 140214 0 None -45 3 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
127051040 140279 0 None -66 3 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 491 12 1 4 5.9 CCCCCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805826 140279 0 None -66 3 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 491 12 1 4 5.9 CCCCCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
127051038 140312 0 None -41 3 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 421 8 1 4 4.1 NC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3806169 140312 0 None -41 3 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 421 8 1 4 4.1 NC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
24861188 199736 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 314 5 2 3 2.8 CNCCc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12 10.1016/j.bmc.2009.09.023
CHEMBL593527 199736 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human 5HT2A receptor expressed in CHO cells assessed as inhibition of (R)-(-)-DOI hydrochloride-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 314 5 2 3 2.8 CNCCc1cccc2[nH]cc(S(=O)(=O)c3ccccc3)c12 10.1016/j.bmc.2009.09.023
129186530 156226 0 None 6 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 426 4 1 9 1.7 Cc1nc2n(c(=O)c1CCN1CCN(c3ncnc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4064609 156226 0 None 6 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 426 4 1 9 1.7 Cc1nc2n(c(=O)c1CCN1CCN(c3ncnc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
156015526 177598 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 514 9 2 3 5.3 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCN(C(=S)NC(C)C)CC2)cc1 10.1021/acs.jmedchem.0c00002
CHEMBL4640741 177598 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assayAntagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay
ChEMBL 514 9 2 3 5.3 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCN(C(=S)NC(C)C)CC2)cc1 10.1021/acs.jmedchem.0c00002
145987659 167249 0 None -3 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 421 5 0 5 3.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4292655 167249 0 None -3 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 421 5 0 5 3.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145963961 164403 0 None -51 6 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4213342 164403 0 None -51 6 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
71528204 86969 0 None -8128 3 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human 5-HT2A receptor assessed as decrease in agonist-induced intracellular calcium mobilization preincubated for 10 mins prior to agonist addition measured by FLIPR analysisAntagonist activity at human 5-HT2A receptor assessed as decrease in agonist-induced intracellular calcium mobilization preincubated for 10 mins prior to agonist addition measured by FLIPR analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
CHEMBL2323579 86969 0 None -8128 3 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human 5-HT2A receptor assessed as decrease in agonist-induced intracellular calcium mobilization preincubated for 10 mins prior to agonist addition measured by FLIPR analysisAntagonist activity at human 5-HT2A receptor assessed as decrease in agonist-induced intracellular calcium mobilization preincubated for 10 mins prior to agonist addition measured by FLIPR analysis
ChEMBL 439 6 1 5 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 10.1021/ml3003814
137630811 161110 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
CHEMBL4082150 161110 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
CHEMBL4117087 161110 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
168291367 191950 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 532 7 1 4 4.7 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)c(Br)c2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5200788 191950 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 532 7 1 4 4.7 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)c(Br)c2)CC1 10.1016/j.ejmech.2022.114246
129186528 157465 0 None -2 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 442 4 0 6 4.2 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2Cl 10.1016/j.bmc.2017.07.040
CHEMBL4079251 157465 0 None -2 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 442 4 0 6 4.2 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2Cl 10.1016/j.bmc.2017.07.040
11519589 200272 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 544 6 2 4 7.4 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1OCc1ccc(Cl)cc1 10.1021/jm9007328
CHEMBL597151 200272 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 544 6 2 4 7.4 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1OCc1ccc(Cl)cc1 10.1021/jm9007328
9931850 205581 7 None - 1 Human 7.9 pIC50 = 7.9 Functional
Compound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptorCompound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptor
ChEMBL 418 8 0 3 5.4 CCC(=O)N(C1CCCCCCC1)C1CCN(CCCOc2ccc(F)cc2)CC1 10.1016/s0960-894x(00)00483-2
CHEMBL81377 205581 7 None - 1 Human 7.9 pIC50 = 7.9 Functional
Compound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptorCompound was evaluated for its inverse agonist activity against 5-hydroxytryptamine 2A receptor
ChEMBL 418 8 0 3 5.4 CCC(=O)N(C1CCCCCCC1)C1CCN(CCCOc2ccc(F)cc2)CC1 10.1016/s0960-894x(00)00483-2
156017237 177761 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 853 21 0 11 8.5 COc1c(OCCOCCOCCOc2ccc(C3CCN(c4ccn5c(CC6CC6)nnc5c4Cl)CC3)cc2)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
CHEMBL4642761 177761 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 853 21 0 11 8.5 COc1c(OCCOCCOCCOc2ccc(C3CCN(c4ccn5c(CC6CC6)nnc5c4Cl)CC3)cc2)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
156017237 177761 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 853 21 0 11 8.5 COc1c(OCCOCCOCCOc2ccc(C3CCN(c4ccn5c(CC6CC6)nnc5c4Cl)CC3)cc2)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
CHEMBL4642761 177761 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 853 21 0 11 8.5 COc1c(OCCOCCOCCOc2ccc(C3CCN(c4ccn5c(CC6CC6)nnc5c4Cl)CC3)cc2)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c01058
168279444 191177 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 488 7 1 4 4.6 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)c(Cl)c2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5188950 191177 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 488 7 1 4 4.6 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)c(Cl)c2)CC1 10.1016/j.ejmech.2022.114246
168285828 191548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 440 5 1 4 4.1 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc3c(c2)CCC(C)(C)O3)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5194545 191548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 440 5 1 4 4.1 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc3c(c2)CCC(C)(C)O3)CC1 10.1016/j.ejmech.2022.114246
162643405 181751 0 None -38 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR methodAntagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR method
ChEMBL 434 6 1 6 3.5 O=c1[nH]c(=O)n(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc12 10.1016/j.ejmech.2020.112572
CHEMBL4777475 181751 0 None -38 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR methodAntagonist activity at 5-HT2A receptor (unknown origin) assessed as decrease in intracellular calcium flux preincubated with calcium followed by compound challenge and measured after 10 mins by FLIPR method
ChEMBL 434 6 1 6 3.5 O=c1[nH]c(=O)n(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc12 10.1016/j.ejmech.2020.112572
145965041 164255 0 None -10 3 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3ccc4ccsc4c3)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4211473 164255 0 None -10 3 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3ccc4ccsc4c3)CC2)n1 10.1016/j.bmcl.2018.01.038
71457756 83902 0 None -66 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 396 5 0 5 4.7 COc1ccccc1C1CCN(c2ccn3c(CC4CC4)nnc3c2Cl)CC1 10.1021/acs.jmedchem.0c01058
CHEMBL2206440 83902 0 None -66 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 396 5 0 5 4.7 COc1ccccc1C1CCN(c2ccn3c(CC4CC4)nnc3c2Cl)CC1 10.1021/acs.jmedchem.0c01058
156011035 177148 0 None -6 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 437 7 0 8 3.3 COc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
CHEMBL4634009 177148 0 None -6 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 437 7 0 8 3.3 COc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
145989181 167228 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2ccc3ccsc3c2)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4292250 167228 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2ccc3ccsc3c2)CC1 10.1016/j.ejmech.2017.12.099
71566778 165206 21 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT2AAntagonist activity at human 5-HT2A
ChEMBL 394 10 1 6 2.7 CCCCOc1c(OC)cc(C(=O)NCC2(N(C)C)CCOCC2)cc1OC 10.1021/acs.jmedchem.7b00956
CHEMBL4228903 165206 21 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT2AAntagonist activity at human 5-HT2A
ChEMBL 394 10 1 6 2.7 CCCCOc1c(OC)cc(C(=O)NCC2(N(C)C)CCOCC2)cc1OC 10.1021/acs.jmedchem.7b00956
71457756 83902 0 None -66 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 396 5 0 5 4.7 COc1ccccc1C1CCN(c2ccn3c(CC4CC4)nnc3c2Cl)CC1 10.1021/acs.jmedchem.0c01058
CHEMBL2206440 83902 0 None -66 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assayAntagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular Ca2+ mobilization incubated for 1 hr by Fluo-4 dye based fluorescence assay
ChEMBL 396 5 0 5 4.7 COc1ccccc1C1CCN(c2ccn3c(CC4CC4)nnc3c2Cl)CC1 10.1021/acs.jmedchem.0c01058
145963830 164123 0 None -3 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2A 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 164123 0 None -3 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) by calcium release assayAntagonist activity at 5-HT2A 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
156015516 177563 0 None -18 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 485 6 0 7 4.1 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Br)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4640409 177563 0 None -18 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 485 6 0 7 4.1 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Br)cccn12 10.1016/j.bmcl.2020.127027
127048532 140232 0 None -3 3 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cc(F)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805262 140232 0 None -3 3 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cc(F)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
145988038 167176 0 None -85 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 413 6 0 5 4.0 CC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4291215 167176 0 None -85 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 413 6 0 5 4.0 CC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
145975393 163774 0 None -14 2 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4205772 163774 0 None -14 2 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
168279444 191177 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 488 7 1 4 4.6 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)c(Cl)c2)CC1 10.1016/j.ejmech.2022.114246
CHEMBL5188950 191177 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrsInverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs
ChEMBL 488 7 1 4 4.6 CN1CCC(N(Cc2ccc(F)cn2)C(=O)NCc2ccc(OCC(F)(F)F)c(Cl)c2)CC1 10.1016/j.ejmech.2022.114246
168295984 192220 0 None 1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2A 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 192220 0 None 1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) incubated for 60 mins followed by 10 mins incubation in dark at room temperature by FLIPR methodAntagonist activity at 5-HT2A 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
122187394 123039 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 367 5 2 6 2.6 OCCN1CCN(c2nc(Nc3ccccc3F)c3ccccc3n2)CC1 10.1016/j.bmcl.2015.07.030
CHEMBL3609165 123039 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting methodAntagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method
ChEMBL 367 5 2 6 2.6 OCCN1CCN(c2nc(Nc3ccccc3F)c3ccccc3n2)CC1 10.1016/j.bmcl.2015.07.030
168280341 191156 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 427 9 1 3 4.7 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CC(N(C)C)C2)cc1 10.1016/j.ejmech.2022.114246
CHEMBL5188595 191156 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 427 9 1 3 4.7 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CC(N(C)C)C2)cc1 10.1016/j.ejmech.2022.114246
127049850 140235 0 None -23 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 469 8 1 4 5.0 CNC(=O)c1ccc(Cl)c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805327 140235 0 None -23 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 469 8 1 4 5.0 CNC(=O)c1ccc(Cl)c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
1524 2181 96 None 1 18 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulationAntagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm401895u
197 2181 96 None 1 18 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulationAntagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm401895u
3822 2181 96 None 1 18 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulationAntagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm401895u
88 2181 96 None 1 18 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulationAntagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm401895u
CHEMBL51 2181 96 None 1 18 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulationAntagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm401895u
DB12465 2181 96 None 1 18 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulationAntagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm401895u
168289739 191847 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 429 8 1 5 3.5 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)nn2)C2CCN(C)CC2)cc1 10.1016/j.ejmech.2022.114246
CHEMBL5199061 191847 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assayAntagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay
ChEMBL 429 8 1 5 3.5 CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)nn2)C2CCN(C)CC2)cc1 10.1016/j.ejmech.2022.114246
127049848 140297 0 None -15 3 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cc(C)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3806047 140297 0 None -15 3 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cc(C)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
156010883 177144 0 None -15 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(Cl)cn12 10.1016/j.bmcl.2020.127027
CHEMBL4633978 177144 0 None -15 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(Cl)cn12 10.1016/j.bmcl.2020.127027
127049863 140252 0 None -1 6 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805518 140252 0 None -1 6 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
156011666 177306 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 409 6 0 7 3.4 O=c1n(CCCCN2CCC(c3cc(F)cc4oncc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
CHEMBL4636764 177306 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assayAntagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay
ChEMBL 409 6 0 7 3.4 O=c1n(CCCCN2CCC(c3cc(F)cc4oncc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
17956720 200212 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 488 4 2 4 6.0 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1OC(F)(F)F 10.1021/jm9007328
CHEMBL596735 200212 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation countingActivity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
ChEMBL 488 4 2 4 6.0 Cn1ncc(Br)c1-c1cc(NC(=O)Nc2ccc(Cl)cc2)ccc1OC(F)(F)F 10.1021/jm9007328
145976348 163741 0 None -3 3 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL 443 8 1 7 3.2 CNC(=O)c1cncc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2018.01.038
CHEMBL4205326 163741 0 None -3 3 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assayAntagonistic activity at human 5-HT2A receptor assessed as calcium flux after 10 mins by FLIPR assay
ChEMBL