Ligand source activities (1 row/activity)





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

3036780 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3036780.0 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
46780481 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
9903970.0 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
CHEMBL504548 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB06216 107587 None 16 Human Functional pAC50 = 9.7 9.7 3 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14476 None 26 Human Functional pAC50 = 6 6.0 -5 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14476 None 26 Human Functional pAC50 = 6 6.0 -5 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102785 None 36 Human Functional pAC50 = 6 6.0 -162 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
16351.0 102785 None 36 Human Functional pAC50 = 6 6.0 -162 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102785 None 36 Human Functional pAC50 = 6 6.0 -162 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB13256 102785 None 36 Human Functional pAC50 = 6 6.0 -162 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5 5.0 -19 17
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 None 21 Human Functional pAC50 = 5 5.0 -19 17
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 None 21 Human Functional pAC50 = 5 5.0 -19 17
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 None 21 Human Functional pAC50 = 5 5.0 -19 17
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 None 42 Human Functional pAC50 = 5 5.0 -933 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 5 5.0 -933 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 5 5.0 -933 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 5 5.0 -933 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 5 5.0 -933 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.0 5.0 -691 14
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 None 46 Human Functional pAC50 = 5.0 5.0 -691 14
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
5358.0 3707 None 46 Human Functional pAC50 = 5.0 5.0 -691 14
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 None 46 Human Functional pAC50 = 5.0 5.0 -691 14
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 None 46 Human Functional pAC50 = 5.0 5.0 -691 14
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 None 46 Human Functional pAC50 = 5.0 5.0 -691 14
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 None 55 Human Functional pAC50 = 5.0 5.0 -23 42
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 None 55 Human Functional pAC50 = 5.0 5.0 -23 42
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 None 55 Human Functional pAC50 = 5.0 5.0 -23 42
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 None 55 Human Functional pAC50 = 5.0 5.0 -23 42
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 None 55 Human Functional pAC50 = 5.0 5.0 -23 42
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 98934 None 37 Human Functional pAC50 = 5.0 5.0 -56 10
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 98934 None 37 Human Functional pAC50 = 5.0 5.0 -56 10
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 98934 None 37 Human Functional pAC50 = 5.0 5.0 -56 10
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 198259 None 39 Human Functional pAC50 = 5.0 5.0 -3 2
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 198259 None 39 Human Functional pAC50 = 5.0 5.0 -3 2
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 None 21 Human Functional pAC50 = 5.0 5.0 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.0 5.0 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.0 5.0 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.0 5.0 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 84720 None 41 Human Functional pAC50 = 5.0 5.0 -2 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 84720 None 41 Human Functional pAC50 = 5.0 5.0 -2 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206466 None 47 Human Functional pAC50 = 5.0 5.0 -10 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206466 None 47 Human Functional pAC50 = 5.0 5.0 -10 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206466 None 47 Human Functional pAC50 = 5.0 5.0 -10 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 27 Human Functional pAC50 = 6.0 6.0 -104 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
26987.0 949 None 27 Human Functional pAC50 = 6.0 6.0 -104 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 27 Human Functional pAC50 = 6.0 6.0 -104 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 27 Human Functional pAC50 = 6.0 6.0 -104 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 27 Human Functional pAC50 = 6.0 6.0 -104 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 27 Human Functional pAC50 = 6.0 6.0 -104 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 6.0 6.0 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 6.0 6.0 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3396.0 1664 None 37 Human Functional pAC50 = 6.0 6.0 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 6.0 6.0 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 6.0 6.0 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 6.0 6.0 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 122423 None 61 Human Functional pAC50 = 5.0 5.0 -1 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 122423 None 61 Human Functional pAC50 = 5.0 5.0 -1 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 70 Human Functional pAC50 = 6.0 6.0 -229 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 70 Human Functional pAC50 = 6.0 6.0 -229 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 70 Human Functional pAC50 = 6.0 6.0 -229 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
60795.0 470 None 70 Human Functional pAC50 = 6.0 6.0 -229 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 70 Human Functional pAC50 = 6.0 6.0 -229 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 70 Human Functional pAC50 = 6.0 6.0 -229 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 115628 None 61 Human Functional pAC50 = 5.9 5.9 -3 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 115628 None 61 Human Functional pAC50 = 5.9 5.9 -3 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 199383 None 50 Human Functional pAC50 = 4.9 4.9 -13 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 199383 None 50 Human Functional pAC50 = 4.9 4.9 -13 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 13 Human Functional pAC50 = 6.9 6.9 -85 21
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 None 13 Human Functional pAC50 = 6.9 6.9 -85 21
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 None 13 Human Functional pAC50 = 6.9 6.9 -85 21
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 None 33 Human Functional pAC50 = 6.9 6.9 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
16363.0 596 None 33 Human Functional pAC50 = 6.9 6.9 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 6.9 6.9 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 6.9 6.9 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 6.9 6.9 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 6.9 6.9 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.9 6.9 -6 43
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
135398737.0 958 None 57 Human Functional pAC50 = 6.9 6.9 -6 43
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.9 6.9 -6 43
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.9 6.9 -6 43
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.9 6.9 -6 43
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.9 6.9 -6 43
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 29284 None 49 Human Functional pAC50 = 5.9 5.9 -141 19
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 29284 None 49 Human Functional pAC50 = 5.9 5.9 -141 19
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4615.0 29284 None 49 Human Functional pAC50 = 5.9 5.9 -141 19
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 29284 None 49 Human Functional pAC50 = 5.9 5.9 -141 19
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB12877 29284 None 49 Human Functional pAC50 = 5.9 5.9 -141 19
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 4.9 4.9 -27 17
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 None 38 Human Functional pAC50 = 4.9 4.9 -27 17
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
5095.0 3370 None 38 Human Functional pAC50 = 4.9 4.9 -27 17
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 None 38 Human Functional pAC50 = 4.9 4.9 -27 17
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 None 38 Human Functional pAC50 = 4.9 4.9 -27 17
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 None 38 Human Functional pAC50 = 4.9 4.9 -27 17
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 111644 None 40 Human Functional pAC50 = 4.9 4.9 -141 23
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 111644 None 40 Human Functional pAC50 = 4.9 4.9 -141 23
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 14493 None 19 Human Functional pAC50 = 4.9 4.9 -1905 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
16960.0 14493 None 19 Human Functional pAC50 = 4.9 4.9 -1905 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14493 None 19 Human Functional pAC50 = 4.9 4.9 -1905 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB00405 14493 None 19 Human Functional pAC50 = 4.9 4.9 -1905 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
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 None 40 Human Functional pAC50 = 4.9 4.9 -97723 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
11504295.0 2923 None 40 Human Functional pAC50 = 4.9 4.9 -97723 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 40 Human Functional pAC50 = 4.9 4.9 -97723 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 40 Human Functional pAC50 = 4.9 4.9 -97723 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 40 Human Functional pAC50 = 4.9 4.9 -97723 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 40 Human Functional pAC50 = 4.9 4.9 -97723 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 4.9 4.9 -1071 6
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
123606.0 352 None 46 Human Functional pAC50 = 4.9 4.9 -1071 6
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 None 46 Human Functional pAC50 = 4.9 4.9 -1071 6
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 None 46 Human Functional pAC50 = 4.9 4.9 -1071 6
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 None 46 Human Functional pAC50 = 4.9 4.9 -1071 6
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 None 46 Human Functional pAC50 = 4.9 4.9 -1071 6
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 142422 None 66 Human Functional pAC50 = 4.9 4.9 -14 14
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 142422 None 66 Human Functional pAC50 = 4.9 4.9 -14 14
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 41527 None 58 Human Functional pAC50 = 4.9 4.9 -11 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 41527 None 58 Human Functional pAC50 = 4.9 4.9 -11 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 106495 None 32 Human Functional pAC50 = 4.9 4.9 -2290 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 106495 None 32 Human Functional pAC50 = 4.9 4.9 -2290 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 141440 None 61 Human Functional pAC50 = 4.9 4.9 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 141440 None 61 Human Functional pAC50 = 4.9 4.9 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 203394 None 56 Human Functional pAC50 = 4.9 4.9 -6 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 203394 None 56 Human Functional pAC50 = 4.9 4.9 -6 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 5.9 5.9 -14 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 5.9 5.9 -14 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 5.9 5.9 -14 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3372.0 1662 None 37 Human Functional pAC50 = 5.9 5.9 -14 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 5.9 5.9 -14 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 37 Human Functional pAC50 = 5.9 5.9 -14 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 35 Human Functional pAC50 = 5.9 5.9 -141 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 35 Human Functional pAC50 = 5.9 5.9 -141 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 35 Human Functional pAC50 = 5.9 5.9 -141 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
941651.0 3806 None 35 Human Functional pAC50 = 5.9 5.9 -141 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 35 Human Functional pAC50 = 5.9 5.9 -141 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 35 Human Functional pAC50 = 5.9 5.9 -141 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.9 4.9 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 28 Human Functional pAC50 = 5.9 5.9 -26 29
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
31101.0 729 None 28 Human Functional pAC50 = 5.9 5.9 -26 29
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 None 28 Human Functional pAC50 = 5.9 5.9 -26 29
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 None 28 Human Functional pAC50 = 5.9 5.9 -26 29
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 None 28 Human Functional pAC50 = 5.9 5.9 -26 29
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 None 28 Human Functional pAC50 = 5.9 5.9 -26 29
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 None 19 Human Functional pAC50 = 6.9 6.9 -12 18
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 None 19 Human Functional pAC50 = 6.9 6.9 -12 18
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 None 19 Human Functional pAC50 = 6.9 6.9 -12 18
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
9681.0 2514 None 19 Human Functional pAC50 = 6.9 6.9 -12 18
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 None 19 Human Functional pAC50 = 6.9 6.9 -12 18
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 None 19 Human Functional pAC50 = 6.9 6.9 -12 18
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 None 42 Human Functional pAC50 = 6.9 6.9 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 6.9 6.9 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 6.9 6.9 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3964.0 2348 None 42 Human Functional pAC50 = 6.9 6.9 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 6.9 6.9 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 6.9 6.9 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 31 Human Functional pAC50 = 5.9 5.9 -1 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 31 Human Functional pAC50 = 5.9 5.9 -1 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 31 Human Functional pAC50 = 5.9 5.9 -1 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 31 Human Functional pAC50 = 5.9 5.9 -1 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 31 Human Functional pAC50 = 5.9 5.9 -1 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
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 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
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 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
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
60857.0 4152 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
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 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
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 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
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 194829 None 40 Human Functional pAC50 = 4.9 4.9 -8 8
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 194829 None 40 Human Functional pAC50 = 4.9 4.9 -8 8
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 194829 None 40 Human Functional pAC50 = 4.9 4.9 -8 8
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 17999 None 26 Human Functional pAC50 = 4.9 4.9 -9 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 17999 None 26 Human Functional pAC50 = 4.9 4.9 -9 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78289 None 22 Human Functional pAC50 = 4.9 4.9 -41 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78289 None 22 Human Functional pAC50 = 4.9 4.9 -41 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 93987 None 66 Human Functional pAC50 = 4.9 4.9 -22 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 93987 None 66 Human Functional pAC50 = 4.9 4.9 -22 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.8 5.8 -173 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.8 5.8 -173 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.8 5.8 -173 35
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15507 None 60 Human Functional pAC50 = 4.8 4.8 -1 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15507 None 60 Human Functional pAC50 = 4.8 4.8 -1 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 31229 None 62 Human Functional pAC50 = 4.8 4.8 -33 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 31229 None 62 Human Functional pAC50 = 4.8 4.8 -33 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 32008 None 48 Human Functional pAC50 = 4.8 4.8 -4466 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 32008 None 48 Human Functional pAC50 = 4.8 4.8 -4466 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 32008 None 48 Human Functional pAC50 = 4.8 4.8 -4466 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78430 None 26 Human Functional pAC50 = 4.8 4.8 -1000 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78430 None 26 Human Functional pAC50 = 4.8 4.8 -1000 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 98179 None 50 Human Functional pAC50 = 4.8 4.8 -213 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 98179 None 50 Human Functional pAC50 = 4.8 4.8 -213 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 17 Human Functional pAC50 = 5.8 5.8 -97 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
1201549.0 597 None 17 Human Functional pAC50 = 5.8 5.8 -97 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 17 Human Functional pAC50 = 5.8 5.8 -97 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 17 Human Functional pAC50 = 5.8 5.8 -97 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 17 Human Functional pAC50 = 5.8 5.8 -97 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 17 Human Functional pAC50 = 5.8 5.8 -97 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 17 Human Functional pAC50 = 5.8 5.8 -97 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 30 Human Functional pAC50 = 5.8 5.8 -3 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 30 Human Functional pAC50 = 5.8 5.8 -3 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 30 Human Functional pAC50 = 5.8 5.8 -3 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 30 Human Functional pAC50 = 5.8 5.8 -3 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 30 Human Functional pAC50 = 5.8 5.8 -3 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 5.8 5.8 -79 39
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 5.8 5.8 -79 39
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3559.0 1911 None 63 Human Functional pAC50 = 5.8 5.8 -79 39
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 5.8 5.8 -79 39
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 5.8 5.8 -79 39
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 5.8 5.8 -79 39
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 69 Human Functional pAC50 = 4.8 4.8 -8912 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 69 Human Functional pAC50 = 4.8 4.8 -8912 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 69 Human Functional pAC50 = 4.8 4.8 -8912 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
65999.0 3776 None 69 Human Functional pAC50 = 4.8 4.8 -8912 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 69 Human Functional pAC50 = 4.8 4.8 -8912 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 69 Human Functional pAC50 = 4.8 4.8 -8912 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 5.8 5.8 -2 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
124087.0 1389 None 72 Human Functional pAC50 = 5.8 5.8 -2 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 5.8 5.8 -2 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 5.8 5.8 -2 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 5.8 5.8 -2 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 5.8 5.8 -2 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 28732 None 28 Human Functional pAC50 = 5.8 5.8 -512 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5440.0 28732 None 28 Human Functional pAC50 = 5.8 5.8 -512 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 28732 None 28 Human Functional pAC50 = 5.8 5.8 -512 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB00372 28732 None 28 Human Functional pAC50 = 5.8 5.8 -512 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 209699 None 30 Human Functional pAC50 = 5.8 5.8 -2 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 209699 None 30 Human Functional pAC50 = 5.8 5.8 -2 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 4.8 4.8 -223 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 4.8 4.8 -223 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 4.8 4.8 -223 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 4.8 4.8 -223 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5775.0 3096 None 36 Human Functional pAC50 = 4.8 4.8 -223 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 4.8 4.8 -223 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 4.8 4.8 -223 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 4.8 4.8 -602 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 4.8 4.8 -602 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 4.8 4.8 -602 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
9913767.0 3578 None 61 Human Functional pAC50 = 4.8 4.8 -602 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 4.8 4.8 -602 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 4.8 4.8 -602 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 61580 None 50 Human Functional pAC50 = 4.8 4.8 -7 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
60606.0 61580 None 50 Human Functional pAC50 = 4.8 4.8 -7 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 61580 None 50 Human Functional pAC50 = 4.8 4.8 -7 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB00758 61580 None 50 Human Functional pAC50 = 4.8 4.8 -7 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 120571 None 49 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 120571 None 49 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 103047 None 29 Human Functional pAC50 = 4.8 4.8 -7 5
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 103047 None 29 Human Functional pAC50 = 4.8 4.8 -7 5
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 None 51 Human Functional pAC50 = 4.8 4.8 -912 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 4.8 4.8 -912 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3100.0 1432 None 51 Human Functional pAC50 = 4.8 4.8 -912 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 4.8 4.8 -912 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 4.8 4.8 -912 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 4.8 4.8 -912 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 4.8 4.8 -912 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78218 None 21 Human Functional pAC50 = 4.8 4.8 -3 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78218 None 21 Human Functional pAC50 = 4.8 4.8 -3 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207971 None 50 Human Functional pAC50 = 4.8 4.8 -29 37
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207971 None 50 Human Functional pAC50 = 4.8 4.8 -29 37
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207971 None 50 Human Functional pAC50 = 4.8 4.8 -29 37
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207349 None 24 Human Functional pAC50 = 4.8 4.8 -15 19
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 207349 None 24 Human Functional pAC50 = 4.8 4.8 -15 19
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 207349 None 24 Human Functional pAC50 = 4.8 4.8 -15 19
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 None 20 Human Functional pAC50 = 5.8 5.8 -316 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 20 Human Functional pAC50 = 5.8 5.8 -316 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 20 Human Functional pAC50 = 5.8 5.8 -316 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
6005.0 445 None 20 Human Functional pAC50 = 5.8 5.8 -316 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 20 Human Functional pAC50 = 5.8 5.8 -316 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 20 Human Functional pAC50 = 5.8 5.8 -316 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 17168 None 30 Human Functional pAC50 = 4.8 4.8 -3 4
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 17168 None 30 Human Functional pAC50 = 4.8 4.8 -3 4
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 97442 None 46 Human Functional pAC50 = 4.8 4.8 -2 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 97442 None 46 Human Functional pAC50 = 4.8 4.8 -2 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 98741 None 64 Human Functional pAC50 = 4.8 4.8 -34 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 98741 None 64 Human Functional pAC50 = 4.8 4.8 -34 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102451 None 54 Human Functional pAC50 = 4.8 4.8 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102451 None 54 Human Functional pAC50 = 4.8 4.8 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 161633 None 72 Human Functional pAC50 = 4.8 4.8 -1 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 161633 None 72 Human Functional pAC50 = 4.8 4.8 -1 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 193531 None 56 Human Functional pAC50 = 4.8 4.8 -380 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 193531 None 56 Human Functional pAC50 = 4.8 4.8 -380 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 99377 None 50 Human Functional pAC50 = 5.8 5.8 -81 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2448.0 99377 None 50 Human Functional pAC50 = 5.8 5.8 -81 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 99377 None 50 Human Functional pAC50 = 5.8 5.8 -81 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB12401 99377 None 50 Human Functional pAC50 = 5.8 5.8 -81 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206037 None 20 Human Functional pAC50 = 5.8 5.8 -199 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206037 None 20 Human Functional pAC50 = 5.8 5.8 -199 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.7 5.7 -3 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.7 5.7 -3 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.7 5.7 -3 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.7 5.7 -3 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.7 5.7 -3 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.7 5.7 -3 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207729 None 57 Human Functional pAC50 = 5.7 5.7 -3 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 4.7 4.7 -9549 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 4.7 4.7 -9549 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 4.7 4.7 -9549 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5717.0 4132 None 63 Human Functional pAC50 = 4.7 4.7 -9549 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 4.7 4.7 -9549 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 63 Human Functional pAC50 = 4.7 4.7 -9549 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14425 None 55 Human Functional pAC50 = 4.7 4.7 -10 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14425 None 55 Human Functional pAC50 = 4.7 4.7 -10 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14505 None 4 Human Functional pAC50 = 4.7 4.7 -117 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
6127.0 14505 None 4 Human Functional pAC50 = 4.7 4.7 -117 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14505 None 4 Human Functional pAC50 = 4.7 4.7 -117 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB13720 14505 None 4 Human Functional pAC50 = 4.7 4.7 -117 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 50235 None 31 Human Functional pAC50 = 4.7 4.7 -47 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 50235 None 31 Human Functional pAC50 = 4.7 4.7 -47 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 50235 None 31 Human Functional pAC50 = 4.7 4.7 -47 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206863 None 31 Human Functional pAC50 = 4.7 4.7 -7079 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2995.0 206863 None 31 Human Functional pAC50 = 4.7 4.7 -7079 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206863 None 31 Human Functional pAC50 = 4.7 4.7 -7079 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206863 None 31 Human Functional pAC50 = 4.7 4.7 -7079 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB01151 206863 None 31 Human Functional pAC50 = 4.7 4.7 -7079 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 178724 None 43 Human Functional pAC50 = 5.7 5.7 -8 19
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 178724 None 43 Human Functional pAC50 = 5.7 5.7 -8 19
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 8.6 8.6 -1 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 8.6 8.6 -1 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5073.0 3331 None 72 Human Functional pAC50 = 8.6 8.6 -1 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 8.6 8.6 -1 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 8.6 8.6 -1 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 72 Human Functional pAC50 = 8.6 8.6 -1 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -3 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -3 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -3 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 11852 None 18 Human Functional pAC50 = 5.7 5.7 -3 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 56283 None 21 Human Functional pAC50 = 5.7 5.7 -194 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3158.0 56283 None 21 Human Functional pAC50 = 5.7 5.7 -194 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 56283 None 21 Human Functional pAC50 = 5.7 5.7 -194 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB01142 56283 None 21 Human Functional pAC50 = 5.7 5.7 -194 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 4.7 4.7 -2 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 4.7 4.7 -2 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 4.7 4.7 -2 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 4.7 4.7 -2 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 4.7 4.7 -2 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 33583 None 70 Human Functional pAC50 = 4.7 4.7 1 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 33583 None 70 Human Functional pAC50 = 4.7 4.7 1 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
CHEMBL5416410 33583 None 70 Human Functional pAC50 = 4.7 4.7 1 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 142422 None 66 Human Functional pAC50 = 4.7 4.7 -14 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 142422 None 66 Human Functional pAC50 = 4.7 4.7 -14 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 24 Human Functional pAC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pAC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pAC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pAC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pAC50 = 6.7 6.7 -17 11
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 None 38 Human Functional pAC50 = 6.7 6.7 -57 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.7 6.7 -57 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.7 6.7 -57 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5709.0 4107 None 38 Human Functional pAC50 = 6.7 6.7 -57 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.7 6.7 -57 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.7 6.7 -57 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
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 172649 None 27 Human Functional pAC50 = 4.7 4.7 -13 3
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 172649 None 27 Human Functional pAC50 = 4.7 4.7 -13 3
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 100668 None 35 Human Functional pAC50 = 4.7 4.7 -22 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 100668 None 35 Human Functional pAC50 = 4.7 4.7 -22 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 106495 None 32 Human Functional pAC50 = 4.7 4.7 -2290 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 106495 None 32 Human Functional pAC50 = 4.7 4.7 -2290 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 4.7 4.7 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 4301 None 35 Human Functional pAC50 = 4.7 4.7 -9 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 4301 None 35 Human Functional pAC50 = 4.7 4.7 -9 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 4301 None 35 Human Functional pAC50 = 4.7 4.7 -9 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 120668 None 8 Human Functional pAC50 = 4.7 4.7 -32 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5311017.0 120668 None 8 Human Functional pAC50 = 4.7 4.7 -32 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 120668 None 8 Human Functional pAC50 = 4.7 4.7 -32 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB00865 120668 None 8 Human Functional pAC50 = 4.7 4.7 -32 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 188375 None 19 Human Functional pAC50 = 4.7 4.7 -8 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 188375 None 19 Human Functional pAC50 = 4.7 4.7 -8 7
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 107137 None 37 Human Functional pAC50 = 5.7 5.7 1 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 107137 None 37 Human Functional pAC50 = 5.7 5.7 1 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.6 7.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
213046.0 2385 None 44 Human Functional pAC50 = 7.6 7.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.6 7.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.6 7.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.6 7.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.6 7.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 24 Human Functional pAC50 = 5.6 5.6 -45 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 24 Human Functional pAC50 = 5.6 5.6 -45 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4768.0 3095 None 24 Human Functional pAC50 = 5.6 5.6 -45 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 24 Human Functional pAC50 = 5.6 5.6 -45 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 24 Human Functional pAC50 = 5.6 5.6 -45 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 24 Human Functional pAC50 = 5.6 5.6 -45 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 5260 None 48 Human Functional pAC50 = 5.6 5.6 1 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 5260 None 48 Human Functional pAC50 = 5.6 5.6 1 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -10232 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3157.0 1470 None 44 Human Functional pAC50 = 4.6 4.6 -10232 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -10232 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -10232 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -10232 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -10232 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 4.6 4.6 -416 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 4.6 4.6 -416 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 4.6 4.6 -416 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
23897.0 2590 None 33 Human Functional pAC50 = 4.6 4.6 -416 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 4.6 4.6 -416 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 4.6 4.6 -416 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.6 4.6 -13489 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
10184665.0 3991 None 42 Human Functional pAC50 = 4.6 4.6 -13489 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.6 4.6 -13489 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.6 4.6 -13489 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.6 4.6 -13489 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.6 4.6 -13489 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.6 6.6 -57 18
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 None 38 Human Functional pAC50 = 6.6 6.6 -57 18
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 None 38 Human Functional pAC50 = 6.6 6.6 -57 18
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
5709.0 4107 None 38 Human Functional pAC50 = 6.6 6.6 -57 18
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 None 38 Human Functional pAC50 = 6.6 6.6 -57 18
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 None 38 Human Functional pAC50 = 6.6 6.6 -57 18
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 None 58 Human Functional pAC50 = 4.6 4.6 -426 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
119570.0 3159 None 58 Human Functional pAC50 = 4.6 4.6 -426 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 4.6 4.6 -426 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 4.6 4.6 -426 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 4.6 4.6 -426 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 4.6 4.6 -426 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 19155 None 57 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 19155 None 57 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 43578 None 39 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 43578 None 39 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78239 None 45 Human Functional pAC50 = 4.6 4.6 -7943 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78239 None 45 Human Functional pAC50 = 4.6 4.6 -7943 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 98934 None 37 Human Functional pAC50 = 4.6 4.6 -56 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 98934 None 37 Human Functional pAC50 = 4.6 4.6 -56 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 98934 None 37 Human Functional pAC50 = 4.6 4.6 -56 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 99367 None 27 Human Functional pAC50 = 4.6 4.6 -39 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 99367 None 27 Human Functional pAC50 = 4.6 4.6 -39 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 5.6 5.6 -549 20
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 None 36 Human Functional pAC50 = 5.6 5.6 -549 20
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 None 36 Human Functional pAC50 = 5.6 5.6 -549 20
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
8969.0 4127 None 36 Human Functional pAC50 = 5.6 5.6 -549 20
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 None 36 Human Functional pAC50 = 5.6 5.6 -549 20
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 None 36 Human Functional pAC50 = 5.6 5.6 -549 20
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 16653 None 45 Human Functional pAC50 = 5.6 5.6 -1 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 16653 None 45 Human Functional pAC50 = 5.6 5.6 -1 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 82440 None 34 Human Functional pAC50 = 5.6 5.6 -46 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 82440 None 34 Human Functional pAC50 = 5.6 5.6 -46 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 110592 None 24 Human Functional pAC50 = 5.6 5.6 -251 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2780.0 110592 None 24 Human Functional pAC50 = 5.6 5.6 -251 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 110592 None 24 Human Functional pAC50 = 5.6 5.6 -251 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB13511 110592 None 24 Human Functional pAC50 = 5.6 5.6 -251 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.6 5.6 -16 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.6 5.6 -16 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.6 5.6 -16 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.6 5.6 -16 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.6 5.6 -16 34
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 5.6 5.6 -20 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 5.6 5.6 -20 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4927.0 3183 None 36 Human Functional pAC50 = 5.6 5.6 -20 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 5.6 5.6 -20 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 5.6 5.6 -20 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 5.6 5.6 -20 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 194796 None 31 Human Functional pAC50 = 4.6 4.6 -7 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 194796 None 31 Human Functional pAC50 = 4.6 4.6 -7 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 5720 None 27 Human Functional pAC50 = 4.6 4.6 -31 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4942.0 5720 None 27 Human Functional pAC50 = 4.6 4.6 -31 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 5720 None 27 Human Functional pAC50 = 4.6 4.6 -31 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB12278 5720 None 27 Human Functional pAC50 = 4.6 4.6 -31 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 53206 None 25 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 53206 None 25 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -457 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -457 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -457 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -457 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 4.6 4.6 -457 27
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 4643 None 51 Human Functional pAC50 = 4.6 4.6 -9 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 4643 None 51 Human Functional pAC50 = 4.6 4.6 -9 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 84819 None 58 Human Functional pAC50 = 4.6 4.6 -2 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 84819 None 58 Human Functional pAC50 = 4.6 4.6 -2 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 187026 None 38 Human Functional pAC50 = 4.6 4.6 -102 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 187026 None 38 Human Functional pAC50 = 4.6 4.6 -102 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 187026 None 38 Human Functional pAC50 = 4.6 4.6 -102 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 157623 None 57 Human Functional pAC50 = 5.6 5.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 157623 None 57 Human Functional pAC50 = 5.6 5.6 -1 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 67 Human Functional pAC50 = 4.6 4.6 -51 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 67 Human Functional pAC50 = 4.6 4.6 -51 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 67 Human Functional pAC50 = 4.6 4.6 -51 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 67 Human Functional pAC50 = 4.6 4.6 -51 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 67 Human Functional pAC50 = 4.6 4.6 -51 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 112646 None 60 Human Functional pAC50 = 4.6 4.6 -91 4
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 112646 None 60 Human Functional pAC50 = 4.6 4.6 -91 4
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 133581 None 40 Human Functional pAC50 = 4.6 4.6 -346 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 133581 None 40 Human Functional pAC50 = 4.6 4.6 -346 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 133581 None 40 Human Functional pAC50 = 4.6 4.6 -346 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 210459 None 52 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 210459 None 52 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15289 None 20 Human Functional pAC50 = 5.5 5.5 -3 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15289 None 20 Human Functional pAC50 = 5.5 5.5 -3 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78221 None 44 Human Functional pAC50 = 5.5 5.5 3 3
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78221 None 44 Human Functional pAC50 = 5.5 5.5 3 3
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78250 None 62 Human Functional pAC50 = 5.5 5.5 -2 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78250 None 62 Human Functional pAC50 = 5.5 5.5 -2 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
33036.0 918 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 42 Human Functional pAC50 = 4.5 4.5 -524 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78302 None 14 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78302 None 14 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 8.5 8.5 2 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 8.5 8.5 2 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
71360.0 2006 None 61 Human Functional pAC50 = 8.5 8.5 2 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 8.5 8.5 2 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 8.5 8.5 2 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 61 Human Functional pAC50 = 8.5 8.5 2 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 51685 None 37 Human Functional pAC50 = 6.5 6.5 -4 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 51685 None 37 Human Functional pAC50 = 6.5 6.5 -4 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 5.5 5.5 -7 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 5.5 5.5 -7 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 5.5 5.5 -7 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5002.0 3256 None 51 Human Functional pAC50 = 5.5 5.5 -7 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 5.5 5.5 -7 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 51 Human Functional pAC50 = 5.5 5.5 -7 29
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 10802 None 64 Human Functional pAC50 = 6.5 6.5 10 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 10802 None 64 Human Functional pAC50 = 6.5 6.5 10 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 209982 None 33 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
19861.0 209982 None 33 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 209982 None 33 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB00719 209982 None 33 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.5 5.5 -5 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.5 5.5 -5 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4917.0 3173 None 38 Human Functional pAC50 = 5.5 5.5 -5 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.5 5.5 -5 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.5 5.5 -5 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.5 5.5 -5 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 6.5 6.5 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 6.5 6.5 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3827.0 2182 None 36 Human Functional pAC50 = 6.5 6.5 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 6.5 6.5 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 6.5 6.5 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 36 Human Functional pAC50 = 6.5 6.5 -5 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 64 Human Functional pAC50 = 6.5 6.5 -53 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 64 Human Functional pAC50 = 6.5 6.5 -53 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4205.0 2540 None 64 Human Functional pAC50 = 6.5 6.5 -53 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 64 Human Functional pAC50 = 6.5 6.5 -53 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 64 Human Functional pAC50 = 6.5 6.5 -53 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 64 Human Functional pAC50 = 6.5 6.5 -53 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 52 Human Functional pAC50 = 5.5 5.5 -3 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 52 Human Functional pAC50 = 5.5 5.5 -3 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 52 Human Functional pAC50 = 5.5 5.5 -3 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 52 Human Functional pAC50 = 5.5 5.5 -3 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 52 Human Functional pAC50 = 5.5 5.5 -3 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14501 None 15 Human Functional pAC50 = 4.5 4.5 -3 4
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
5906.0 14501 None 15 Human Functional pAC50 = 4.5 4.5 -3 4
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 14501 None 15 Human Functional pAC50 = 4.5 4.5 -3 4
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
DB00610 14501 None 15 Human Functional pAC50 = 4.5 4.5 -3 4
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 15305 None 29 Human Functional pAC50 = 5.4 5.4 -2 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15305 None 29 Human Functional pAC50 = 5.4 5.4 -2 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15305 None 29 Human Functional pAC50 = 5.4 5.4 -2 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 189330 None 32 Human Functional pAC50 = 5.4 5.4 -13 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 189330 None 32 Human Functional pAC50 = 5.4 5.4 -13 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 189330 None 32 Human Functional pAC50 = 5.4 5.4 -13 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 7.4 7.4 6 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 7.4 7.4 6 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
27400.0 3134 None 58 Human Functional pAC50 = 7.4 7.4 6 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 7.4 7.4 6 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 7.4 7.4 6 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 7.4 7.4 6 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 5.4 5.4 -338 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 5.4 5.4 -338 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 5.4 5.4 -338 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 5.4 5.4 -338 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 58 Human Functional pAC50 = 5.4 5.4 -338 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207084 None 54 Human Functional pAC50 = 5.4 5.4 -239 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4066.0 207084 None 54 Human Functional pAC50 = 5.4 5.4 -239 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207084 None 54 Human Functional pAC50 = 5.4 5.4 -239 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB01071 207084 None 54 Human Functional pAC50 = 5.4 5.4 -239 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 5.4 5.4 -724 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2585.0 803 None 59 Human Functional pAC50 = 5.4 5.4 -724 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 5.4 5.4 -724 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 5.4 5.4 -724 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 5.4 5.4 -724 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 5.4 5.4 -724 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 35070 None 5 Human Functional pAC50 = 5.4 5.4 -3 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 35070 None 5 Human Functional pAC50 = 5.4 5.4 -3 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 35070 None 5 Human Functional pAC50 = 5.4 5.4 -3 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 28 Human Functional pAC50 = 8.3 8.3 -2 25
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 None 28 Human Functional pAC50 = 8.3 8.3 -2 25
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 None 28 Human Functional pAC50 = 8.3 8.3 -2 25
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 None 28 Human Functional pAC50 = 8.3 8.3 -2 25
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 None 28 Human Functional pAC50 = 8.3 8.3 -2 25
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 None 6 Human Functional pAC50 = 7.4 7.4 -54 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 6 Human Functional pAC50 = 7.4 7.4 -54 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 6 Human Functional pAC50 = 7.4 7.4 -54 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
8223.0 1582 None 6 Human Functional pAC50 = 7.4 7.4 -54 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 6 Human Functional pAC50 = 7.4 7.4 -54 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 6 Human Functional pAC50 = 7.4 7.4 -54 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78295 None 23 Human Functional pAC50 = 6.4 6.4 -3 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78295 None 23 Human Functional pAC50 = 6.4 6.4 -3 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206077 None 58 Human Functional pAC50 = 5.4 5.4 -93 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206077 None 58 Human Functional pAC50 = 5.4 5.4 -93 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 40 Human Functional pAC50 = 5.4 5.4 -2570 23
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 None 40 Human Functional pAC50 = 5.4 5.4 -2570 23
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 None 40 Human Functional pAC50 = 5.4 5.4 -2570 23
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 None 40 Human Functional pAC50 = 5.4 5.4 -2570 23
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 None 40 Human Functional pAC50 = 5.4 5.4 -2570 23
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 14500 None 28 Human Functional pAC50 = 5.4 5.4 1 4
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14500 None 28 Human Functional pAC50 = 5.4 5.4 1 4
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 9159 None 27 Human Functional pAC50 = 5.4 5.4 -120 21
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 9159 None 27 Human Functional pAC50 = 5.4 5.4 -120 21
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 None 50 Human Functional pAC50 = 6.3 6.3 -138 17
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 None 50 Human Functional pAC50 = 6.3 6.3 -138 17
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
59227.0 3372 None 50 Human Functional pAC50 = 6.3 6.3 -138 17
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 None 50 Human Functional pAC50 = 6.3 6.3 -138 17
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 None 50 Human Functional pAC50 = 6.3 6.3 -138 17
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 None 50 Human Functional pAC50 = 6.3 6.3 -138 17
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 None 45 Human Functional pAC50 = 5.3 5.3 -190 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2267.0 559 None 45 Human Functional pAC50 = 5.3 5.3 -190 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 45 Human Functional pAC50 = 5.3 5.3 -190 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 45 Human Functional pAC50 = 5.3 5.3 -190 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 45 Human Functional pAC50 = 5.3 5.3 -190 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 45 Human Functional pAC50 = 5.3 5.3 -190 14
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 6.3 6.3 -23 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 6.3 6.3 -23 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 6.3 6.3 -23 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 6.3 6.3 -23 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 59 Human Functional pAC50 = 6.3 6.3 -23 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.3 5.3 -72 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.3 5.3 -72 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.3 5.3 -72 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
644019.0 788 None 26 Human Functional pAC50 = 5.3 5.3 -72 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.3 5.3 -72 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.3 5.3 -72 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 194838 None 50 Human Functional pAC50 = 5.3 5.3 -6 37
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 194838 None 50 Human Functional pAC50 = 5.3 5.3 -6 37
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 25 Human Functional pAC50 = 6.3 6.3 -154 17
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 None 25 Human Functional pAC50 = 6.3 6.3 -154 17
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 None 25 Human Functional pAC50 = 6.3 6.3 -154 17
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 None 25 Human Functional pAC50 = 6.3 6.3 -154 17
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 None 25 Human Functional pAC50 = 6.3 6.3 -154 17
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 41735 None 12 Human Functional pAC50 = 5.3 5.3 -251 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5284550.0 41735 None 12 Human Functional pAC50 = 5.3 5.3 -251 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
CHEMBL108947 41735 None 12 Human Functional pAC50 = 5.3 5.3 -251 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 41735 None 12 Human Functional pAC50 = 5.3 5.3 -251 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB09167 41735 None 12 Human Functional pAC50 = 5.3 5.3 -251 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 4402 None 68 Human Functional pAC50 = 5.3 5.3 -691 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 4402 None 68 Human Functional pAC50 = 5.3 5.3 -691 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14115 None 19 Human Functional pAC50 = 4.3 4.3 -19 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 14115 None 19 Human Functional pAC50 = 4.3 4.3 -19 5
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 7.3 7.3 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
135398745.0 2914 None 65 Human Functional pAC50 = 7.3 7.3 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 7.3 7.3 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 7.3 7.3 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 7.3 7.3 -1 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 32 Human Functional pAC50 = 6.3 6.3 -107 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 32 Human Functional pAC50 = 6.3 6.3 -107 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 32 Human Functional pAC50 = 6.3 6.3 -107 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4543.0 2866 None 32 Human Functional pAC50 = 6.3 6.3 -107 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 32 Human Functional pAC50 = 6.3 6.3 -107 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 32 Human Functional pAC50 = 6.3 6.3 -107 32
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 194927 None 32 Human Functional pAC50 = 6.3 6.3 -4 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5311507.0 194927 None 32 Human Functional pAC50 = 6.3 6.3 -4 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 194927 None 32 Human Functional pAC50 = 6.3 6.3 -4 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB01624 194927 None 32 Human Functional pAC50 = 6.3 6.3 -4 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 208825 None 14 Human Functional pAC50 = 5.3 5.3 -1 6
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
3337.0 208825 None 14 Human Functional pAC50 = 5.3 5.3 -1 6
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 208825 None 14 Human Functional pAC50 = 5.3 5.3 -1 6
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 208825 None 14 Human Functional pAC50 = 5.3 5.3 -1 6
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 208825 None 14 Human Functional pAC50 = 5.3 5.3 -1 6
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 208825 None 14 Human Functional pAC50 = 5.3 5.3 -1 6
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
DB00574 208825 None 14 Human Functional pAC50 = 5.3 5.3 -1 6
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 None 65 Human Functional pAC50 = 6.3 6.3 -38 24
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3151.0 1462 None 65 Human Functional pAC50 = 6.3 6.3 -38 24
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 6.3 6.3 -38 24
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 6.3 6.3 -38 24
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 6.3 6.3 -38 24
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 65 Human Functional pAC50 = 6.3 6.3 -38 24
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 96601 None 25 Human Functional pAC50 = 6.3 6.3 -1 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 96601 None 25 Human Functional pAC50 = 6.3 6.3 -1 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 84404 None 3 Human Functional pAC50 = 5.3 5.3 -3090 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
55645.0 84404 None 3 Human Functional pAC50 = 5.3 5.3 -3090 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 84404 None 3 Human Functional pAC50 = 5.3 5.3 -3090 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.2 6.2 -47 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.2 6.2 -47 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.2 6.2 -47 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4748.0 3057 None 57 Human Functional pAC50 = 6.2 6.2 -47 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.2 6.2 -47 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 57 Human Functional pAC50 = 6.2 6.2 -47 25
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.2 5.2 -19 17
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 None 21 Human Functional pAC50 = 5.2 5.2 -19 17
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 None 21 Human Functional pAC50 = 5.2 5.2 -19 17
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 None 21 Human Functional pAC50 = 5.2 5.2 -19 17
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 204590 None 44 Human Functional pAC50 = 5.2 5.2 -602 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
9429.0 204590 None 44 Human Functional pAC50 = 5.2 5.2 -602 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 204590 None 44 Human Functional pAC50 = 5.2 5.2 -602 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB01622 204590 None 44 Human Functional pAC50 = 5.2 5.2 -602 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 178333 None 41 Human Functional pAC50 = 5.2 5.2 -9 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 178333 None 41 Human Functional pAC50 = 5.2 5.2 -9 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.2 5.2 -7 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.2 5.2 -7 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3658.0 1957 None 46 Human Functional pAC50 = 5.2 5.2 -7 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.2 5.2 -7 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.2 5.2 -7 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.2 5.2 -7 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.2 5.2 -7 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.2 6.2 -112 12
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 None 43 Human Functional pAC50 = 6.2 6.2 -112 12
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
3519.0 1889 None 43 Human Functional pAC50 = 6.2 6.2 -112 12
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 None 43 Human Functional pAC50 = 6.2 6.2 -112 12
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 None 43 Human Functional pAC50 = 6.2 6.2 -112 12
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 None 43 Human Functional pAC50 = 6.2 6.2 -112 12
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 None 26 Human Functional pAC50 = 5.2 5.2 -501 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3042.0 1414 None 26 Human Functional pAC50 = 5.2 5.2 -501 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.2 5.2 -501 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.2 5.2 -501 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.2 5.2 -501 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 26 Human Functional pAC50 = 5.2 5.2 -501 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 41 Human Functional pAC50 = 7.2 7.2 -4 12
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 None 41 Human Functional pAC50 = 7.2 7.2 -4 12
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 None 41 Human Functional pAC50 = 7.2 7.2 -4 12
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
54746.0 778 None 41 Human Functional pAC50 = 7.2 7.2 -4 12
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 None 41 Human Functional pAC50 = 7.2 7.2 -4 12
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 None 41 Human Functional pAC50 = 7.2 7.2 -4 12
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 205585 None 33 Human Functional pAC50 = 5.2 5.2 -3 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 205585 None 33 Human Functional pAC50 = 5.2 5.2 -3 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 84404 None 3 Human Functional pAC50 = 5.2 5.2 -3090 11
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
55645.0 84404 None 3 Human Functional pAC50 = 5.2 5.2 -3090 11
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 84404 None 3 Human Functional pAC50 = 5.2 5.2 -3090 11
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 None 70 Human Functional pAC50 = 6.2 6.2 -229 33
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 None 70 Human Functional pAC50 = 6.2 6.2 -229 33
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 None 70 Human Functional pAC50 = 6.2 6.2 -229 33
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
60795.0 470 None 70 Human Functional pAC50 = 6.2 6.2 -229 33
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 None 70 Human Functional pAC50 = 6.2 6.2 -229 33
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 None 70 Human Functional pAC50 = 6.2 6.2 -229 33
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 None 47 Human Functional pAC50 = 7.2 7.2 3 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 47 Human Functional pAC50 = 7.2 7.2 3 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 47 Human Functional pAC50 = 7.2 7.2 3 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
60854.0 4143 None 47 Human Functional pAC50 = 7.2 7.2 3 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 47 Human Functional pAC50 = 7.2 7.2 3 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 47 Human Functional pAC50 = 7.2 7.2 3 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 208853 None 39 Human Functional pAC50 = 5.2 5.2 -10 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 208853 None 39 Human Functional pAC50 = 5.2 5.2 -10 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15398 None 50 Human Functional pAC50 = 5.2 5.2 -2 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15398 None 50 Human Functional pAC50 = 5.2 5.2 -2 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 15398 None 50 Human Functional pAC50 = 5.2 5.2 -2 10
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 89164 None 10 Human Functional pAC50 = 6.2 6.2 -52 13
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 89164 None 10 Human Functional pAC50 = 6.2 6.2 -52 13
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 154946 None 18 Human Functional pAC50 = 5.2 5.2 -10 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 154946 None 18 Human Functional pAC50 = 5.2 5.2 -10 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 14 Human Functional pAC50 = 8.1 8.1 -1 17
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 None 14 Human Functional pAC50 = 8.1 8.1 -1 17
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 None 14 Human Functional pAC50 = 8.1 8.1 -1 17
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
8226.0 2509 None 14 Human Functional pAC50 = 8.1 8.1 -1 17
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 None 14 Human Functional pAC50 = 8.1 8.1 -1 17
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 None 14 Human Functional pAC50 = 8.1 8.1 -1 17
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 None 33 Human Functional pAC50 = 7.2 7.2 -4 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 7.2 7.2 -4 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 7.2 7.2 -4 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4184.0 2532 None 33 Human Functional pAC50 = 7.2 7.2 -4 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 7.2 7.2 -4 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 33 Human Functional pAC50 = 7.2 7.2 -4 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78202 None 29 Human Functional pAC50 = 7.2 7.2 -1 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
68867.0 78202 None 29 Human Functional pAC50 = 7.2 7.2 -1 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 78202 None 29 Human Functional pAC50 = 7.2 7.2 -1 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB08810 78202 None 29 Human Functional pAC50 = 7.2 7.2 -1 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 48 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2726.0 919 None 48 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 48 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 48 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 48 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 48 Human Functional pAC50 = 6.2 6.2 -6 42
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
189562 2757 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
189562.0 2757 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
71301.0 2757 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
9844194 2757 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
9844194.0 2757 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
CHEMBL2365658 2757 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
CHEMBL3526436 2757 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 41 Human Functional pAC50 = 5.2 5.2 -2344 23
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 34 Human Functional pAC50 = 6.1 6.1 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 34 Human Functional pAC50 = 6.1 6.1 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 34 Human Functional pAC50 = 6.1 6.1 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5533.0 3853 None 34 Human Functional pAC50 = 6.1 6.1 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 34 Human Functional pAC50 = 6.1 6.1 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 34 Human Functional pAC50 = 6.1 6.1 -3 21
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 121354 None 36 Human Functional pAC50 = 5.1 5.1 -301 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 121354 None 36 Human Functional pAC50 = 5.1 5.1 -301 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -27 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -27 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5095.0 3370 None 38 Human Functional pAC50 = 5.1 5.1 -27 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -27 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -27 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -27 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 23 Human Functional pAC50 = 5.1 5.1 -234 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 23 Human Functional pAC50 = 5.1 5.1 -234 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5587.0 3863 None 23 Human Functional pAC50 = 5.1 5.1 -234 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 23 Human Functional pAC50 = 5.1 5.1 -234 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 23 Human Functional pAC50 = 5.1 5.1 -234 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 23 Human Functional pAC50 = 5.1 5.1 -234 9
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 52504 None 58 Human Functional pAC50 = 5.1 5.1 -4 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 52504 None 58 Human Functional pAC50 = 5.1 5.1 -4 2
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 44861 None 29 Human Functional pAC50 = 5.1 5.1 -128 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 44861 None 29 Human Functional pAC50 = 5.1 5.1 -128 12
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -7 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -7 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -7 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
5566.0 3860 None 43 Human Functional pAC50 = 6.1 6.1 -7 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -7 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -7 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -7 28
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 46 Human Functional pAC50 = 5.1 5.1 -56 8
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 None 46 Human Functional pAC50 = 5.1 5.1 -56 8
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
5078.0 3334 None 46 Human Functional pAC50 = 5.1 5.1 -56 8
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 None 46 Human Functional pAC50 = 5.1 5.1 -56 8
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 None 46 Human Functional pAC50 = 5.1 5.1 -56 8
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 None 46 Human Functional pAC50 = 5.1 5.1 -56 8
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 None 60 Human Functional pAC50 = 7.1 7.1 1 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 60 Human Functional pAC50 = 7.1 7.1 1 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 60 Human Functional pAC50 = 7.1 7.1 1 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2170.0 403 None 60 Human Functional pAC50 = 7.1 7.1 1 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 60 Human Functional pAC50 = 7.1 7.1 1 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 60 Human Functional pAC50 = 7.1 7.1 1 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.1 7.1 -3 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.1 7.1 -3 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.1 7.1 -3 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.1 7.1 -3 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 7.1 7.1 -3 22
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -173 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2477.0 745 None 38 Human Functional pAC50 = 5.1 5.1 -173 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -173 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -173 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -173 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 5.1 5.1 -173 20
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 5.1 5.1 -141 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 5.1 5.1 -141 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 5.1 5.1 -141 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 5.1 5.1 -141 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 5.1 5.1 -141 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 5.1 5.1 -141 6
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102913 None 65 Human Functional pAC50 = 5.1 5.1 -48 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
3191.0 102913 None 65 Human Functional pAC50 = 5.1 5.1 -48 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102913 None 65 Human Functional pAC50 = 5.1 5.1 -48 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB11742 102913 None 65 Human Functional pAC50 = 5.1 5.1 -48 33
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 7074 None 25 Human Functional pAC50 = 6.1 6.1 -199 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
17676.0 7074 None 25 Human Functional pAC50 = 6.1 6.1 -199 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 7074 None 25 Human Functional pAC50 = 6.1 6.1 -199 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 7074 None 25 Human Functional pAC50 = 6.1 6.1 -199 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB01063 7074 None 25 Human Functional pAC50 = 6.1 6.1 -199 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.1 5.1 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.1 5.1 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.1 5.1 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 21 Human Functional pAC50 = 5.1 5.1 -19 17
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 19421 None 48 Human Functional pAC50 = 5.1 5.1 -4 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 19421 None 48 Human Functional pAC50 = 5.1 5.1 -4 11
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -123 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -123 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2801.0 954 None 43 Human Functional pAC50 = 6.1 6.1 -123 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -123 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -123 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 43 Human Functional pAC50 = 6.1 6.1 -123 36
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.0 6.0 -158 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.0 6.0 -158 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.0 6.0 -158 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2160.0 401 None 38 Human Functional pAC50 = 6.0 6.0 -158 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.0 6.0 -158 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 38 Human Functional pAC50 = 6.0 6.0 -158 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 34231 None 58 Human Functional pAC50 = 5.0 5.0 -165 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
4418.0 34231 None 58 Human Functional pAC50 = 5.0 5.0 -165 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 34231 None 58 Human Functional pAC50 = 5.0 5.0 -165 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB12092 34231 None 58 Human Functional pAC50 = 5.0 5.0 -165 18
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 12618 None 11 Human Functional pAC50 = 6.0 6.0 3 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 12618 None 11 Human Functional pAC50 = 6.0 6.0 3 26
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 18461 None 59 Human Functional pAC50 = 5.0 5.0 2 3
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 18461 None 59 Human Functional pAC50 = 5.0 5.0 2 3
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 162321 None 58 Human Functional pAC50 = 5.0 5.0 -2 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 162321 None 58 Human Functional pAC50 = 5.0 5.0 -2 8
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 6.0 6.0 -6 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 6.0 6.0 -6 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 6.0 6.0 -6 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 6.0 6.0 -6 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 44 Human Functional pAC50 = 6.0 6.0 -6 38
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206050 None 27 Human Functional pAC50 = 6.0 6.0 -9 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
2895.0 206050 None 27 Human Functional pAC50 = 6.0 6.0 -9 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 206050 None 27 Human Functional pAC50 = 6.0 6.0 -9 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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
DB00924 206050 None 27 Human Functional pAC50 = 6.0 6.0 -9 15
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102826 None 36 Human Functional pAC50 = 5.0 5.0 -1380 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102826 None 36 Human Functional pAC50 = 5.0 5.0 -1380 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 102826 None 36 Human Functional pAC50 = 5.0 5.0 -1380 16
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 59901 None 35 Human Functional pAC50 = 5.0 5.0 -4 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 59901 None 35 Human Functional pAC50 = 5.0 5.0 -4 13
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 32 Human Functional pAC50 = 7.0 7.0 -177 24
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 None 32 Human Functional pAC50 = 7.0 7.0 -177 24
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 None 32 Human Functional pAC50 = 7.0 7.0 -177 24
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
4636.0 2981 None 32 Human Functional pAC50 = 7.0 7.0 -177 24
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 None 32 Human Functional pAC50 = 7.0 7.0 -177 24
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 None 32 Human Functional pAC50 = 7.0 7.0 -177 24
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 207985 None 33 Human Functional pAC50 = 5.0 5.0 -14 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207985 None 33 Human Functional pAC50 = 5.0 5.0 -14 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 207985 None 33 Human Functional pAC50 = 5.0 5.0 -14 30
Antagonist activity at human HTR2A in an in vitro cell-based assay 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 None 13 Human Functional pAC50 = 6 6.0 -100 29
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
10531.0 1420 None 13 Human Functional pAC50 = 6 6.0 -100 29
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 None 13 Human Functional pAC50 = 6 6.0 -100 29
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 None 13 Human Functional pAC50 = 6 6.0 -100 29
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 None 13 Human Functional pAC50 = 6 6.0 -100 29
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 None 13 Human Functional pAC50 = 6 6.0 -100 29
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 None 45 Human Functional pEC50 = 9.6 9.6 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5202 139 None 45 Human Functional pEC50 = 9.6 9.6 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
CHEMBL39 139 None 45 Human Functional pEC50 = 9.6 9.6 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
DB08839 139 None 45 Human Functional pEC50 = 9.6 9.6 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
5202 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
CHEMBL39 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.1c00694
DB08839 139 None 45 Human Functional pEC50 = 9.5 9.5 -15 26
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 191902 None 0 Human Functional pEC50 = 9.3 9.3 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 191902 None 0 Human Functional pEC50 = 9.3 9.3 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 191902 None 0 Human Functional pEC50 = 9.3 9.3 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 191902 None 0 Human Functional pEC50 = 9.3 9.3 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 65 Human Functional pEC50 = 9.3 9.3 6309 3
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 None 65 Human Functional pEC50 = 9.3 9.3 6309 3
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 None 65 Human Functional pEC50 = 9.3 9.3 6309 3
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Human Functional pEC50 = 9.3 9.3 -15 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Mouse Functional pEC50 = 9.3 9.3 2 26
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 None 45 Human Functional pEC50 = 9.2 9.2 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
5202 139 None 45 Human Functional pEC50 = 9.2 9.2 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
CHEMBL39 139 None 45 Human Functional pEC50 = 9.2 9.2 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
DB08839 139 None 45 Human Functional pEC50 = 9.2 9.2 -15 26
Partial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assayPartial agonist activity at human 5-HT2AR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.3c00454
11247569 201876 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 201876 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 None 61 Human Functional pEC50 = 9.0 9.0 1 18
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 None 61 Human Functional pEC50 = 9.0 9.0 1 18
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 None 61 Human Functional pEC50 = 9.0 9.0 1 18
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
3822.0 2181 None 61 Human Functional pEC50 = 9.0 9.0 1 18
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 None 61 Human Functional pEC50 = 9.0 9.0 1 18
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 None 61 Human Functional pEC50 = 9.0 9.0 1 18
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 None 61 Human Functional pEC50 = 9.0 9.0 1 18
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 None 45 Human Functional pEC50 = 9.0 9.0 -15 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -15 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -15 26
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 None 45 Human Functional pEC50 = 9.0 9.0 -15 26
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
5 139 None 45 Human Functional pEC50 = 8.9 8.9 -15 26
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
5202 139 None 45 Human Functional pEC50 = 8.9 8.9 -15 26
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
CHEMBL39 139 None 45 Human Functional pEC50 = 8.9 8.9 -15 26
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
DB08839 139 None 45 Human Functional pEC50 = 8.9 8.9 -15 26
Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
439280 120083 None 57 Human Functional pEC50 = 8.9 8.9 -9 9
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 120083 None 57 Human Functional pEC50 = 8.9 8.9 -9 9
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 120083 None 57 Human Functional pEC50 = 8.9 8.9 -9 9
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 192015 None 0 Human Functional pEC50 = 8.8 8.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192015 None 0 Human Functional pEC50 = 8.8 8.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192015 None 0 Human Functional pEC50 = 8.8 8.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192015 None 0 Human Functional pEC50 = 8.8 8.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 None 45 Human Functional pEC50 = 8.8 8.8 -15 26
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 193118 None 4 Human Functional pEC50 = 8.8 8.8 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 193118 None 4 Human Functional pEC50 = 8.8 8.8 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 193118 None 4 Human Functional pEC50 = 8.8 8.8 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
4376990 193118 None 4 Human Functional pEC50 = 8.8 8.8 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 193118 None 4 Human Functional pEC50 = 8.8 8.8 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 193118 None 4 Human Functional pEC50 = 8.8 8.8 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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 None 16 Human Functional pEC50 = 8.8 8.8 3 12
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
145 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
1832 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
CHEMBL7257 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
DB14010 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
5 139 None 45 Human Functional pEC50 = 8.7 8.7 -15 26
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 None 45 Human Functional pEC50 = 8.7 8.7 -15 26
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 None 45 Human Functional pEC50 = 8.7 8.7 -15 26
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 None 45 Human Functional pEC50 = 8.7 8.7 -15 26
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 120083 None 57 Human Functional pEC50 = 8.7 8.7 -9 9
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 120083 None 57 Human Functional pEC50 = 8.7 8.7 -9 9
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 120083 None 57 Human Functional pEC50 = 8.7 8.7 -9 9
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 190088 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 190088 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 89105 None 0 Human Functional pEC50 = 8 8.0 -17 3
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 89105 None 0 Human Functional pEC50 = 8 8.0 -17 3
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 89105 None 0 Human Functional pEC50 = 8 8.0 -17 3
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 94880 None 0 Human Functional pEC50 = 8 8.0 -2 3
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 94880 None 0 Human Functional pEC50 = 8 8.0 -2 3
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 121837 None 0 Human Functional pEC50 = 8.0 8.0 20 2
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 121837 None 0 Human Functional pEC50 = 8.0 8.0 20 2
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 62519 None 0 Human Functional pEC50 = 7 7.0 -15 3
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 62519 None 0 Human Functional pEC50 = 7 7.0 -15 3
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 63959 None 17 Human Functional pEC50 = 7 7.0 -7 3
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 63959 None 17 Human Functional pEC50 = 7 7.0 -7 3
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 94909 None 0 Human Functional pEC50 = 7 7.0 -12 3
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 94909 None 0 Human Functional pEC50 = 7 7.0 -12 3
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 94966 None 0 Human Functional pEC50 = 7 7.0 -10 3
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 94966 None 0 Human Functional pEC50 = 7 7.0 -10 3
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 154787 None 2 Human Functional pEC50 = 7 7.0 -1 3
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 154787 None 2 Human Functional pEC50 = 7 7.0 -1 3
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 62519 None 0 Human Functional pEC50 = 7 7.0 -15 3
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 62519 None 0 Human Functional pEC50 = 7 7.0 -15 3
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 63787 None 0 Human Functional pEC50 = 7 7.0 -12 3
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 63787 None 0 Human Functional pEC50 = 7 7.0 -12 3
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 166244 None 0 Human Functional pEC50 = 7 7.0 -9 3
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 166244 None 0 Human Functional pEC50 = 7 7.0 -9 3
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 192911 None 0 Human Functional pEC50 = 6 6.0 - 1
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 192911 None 0 Human Functional pEC50 = 6 6.0 - 1
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 192911 None 0 Human Functional pEC50 = 6 6.0 - 1
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 94911 None 2 Human Functional pEC50 = 6 6.0 -251 2
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 94911 None 2 Human Functional pEC50 = 6 6.0 -251 2
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 164186 None 0 Human Functional pEC50 = 4 4.0 -1621 3
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 164186 None 0 Human Functional pEC50 = 4 4.0 -1621 3
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 164853 None 0 Human Functional pEC50 = 4 4.0 -309 3
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 164853 None 0 Human Functional pEC50 = 4 4.0 -309 3
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 120737 None 0 Human Functional pEC50 = 6 6.0 -15 3
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 120737 None 0 Human Functional pEC50 = 6 6.0 -15 3
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 120737 None 0 Human Functional pEC50 = 6 6.0 -15 3
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 120729 None 0 Human Functional pEC50 = 6.0 6.0 -93 3
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 120729 None 0 Human Functional pEC50 = 6.0 6.0 -93 3
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 120729 None 0 Human Functional pEC50 = 6.0 6.0 -93 3
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 91146 None 0 Human Functional pEC50 = 6.0 6.0 -85 2
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 91146 None 0 Human Functional pEC50 = 6.0 6.0 -85 2
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 192973 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192973 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192973 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 91149 None 0 Human Functional pEC50 = 6.0 6.0 -74 2
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 91149 None 0 Human Functional pEC50 = 6.0 6.0 -74 2
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
168941703 196195 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 227 1 1 2 2.6 Cc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5418595 196195 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 227 1 1 2 2.6 Cc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
11176570 91154 None 1 Human Functional pEC50 = 7.0 7.0 -6 2
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 91154 None 1 Human Functional pEC50 = 7.0 7.0 -6 2
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 192973 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192973 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192973 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 207891 None 0 Human Functional pEC50 = 6.0 6.0 -21 3
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 207891 None 0 Human Functional pEC50 = 6.0 6.0 -21 3
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 91131 None 0 Human Functional pEC50 = 7.0 7.0 -6 2
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 91131 None 0 Human Functional pEC50 = 7.0 7.0 -6 2
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 138440 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
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 138440 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
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 138440 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
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 190232 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 190232 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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
168941477 194997 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 229 2 2 3 1.9 COc1cccc2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5394639 194997 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 229 2 2 3 1.9 COc1cccc2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
44412405 77810 None 0 Human Functional pEC50 = 6.0 6.0 -5 3
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 77810 None 0 Human Functional pEC50 = 6.0 6.0 -5 3
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 138440 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
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 138440 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
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 138440 None 0 Human Functional pEC50 = 6.0 6.0 -7 2
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 91130 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 91130 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
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 183729 None 0 Human Functional pEC50 = 7.0 7.0 -16 3
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 183729 None 0 Human Functional pEC50 = 7.0 7.0 -16 3
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 183729 None 0 Human Functional pEC50 = 7.0 7.0 -16 3
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 183729 None 0 Human Functional pEC50 = 7.0 7.0 -16 3
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 183729 None 0 Human Functional pEC50 = 7.0 7.0 -16 3
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 183729 None 0 Human Functional pEC50 = 7.0 7.0 -16 3
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 183788 None 0 Human Functional pEC50 = 7.0 7.0 -42 3
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 183788 None 0 Human Functional pEC50 = 7.0 7.0 -42 3
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 183788 None 0 Human Functional pEC50 = 7.0 7.0 -42 3
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 199847 None 0 Human Functional pEC50 = 6.0 6.0 -23 2
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 199847 None 0 Human Functional pEC50 = 6.0 6.0 -23 2
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 None 45 Human Functional pEC50 = 8.0 8.0 -15 26
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 None 45 Human Functional pEC50 = 8.0 8.0 -15 26
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 None 45 Human Functional pEC50 = 8.0 8.0 -15 26
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 None 45 Human Functional pEC50 = 8.0 8.0 -15 26
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 121856 None 1 Human Functional pEC50 = 8.0 8.0 - 1
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 121856 None 1 Human Functional pEC50 = 8.0 8.0 - 1
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 121857 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 121857 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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
168941574 195420 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2c(C3=CCCNC3)n[nH]c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5403370 195420 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2c(C3=CCCNC3)n[nH]c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5080051 217150 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 102034 None 22 Human Functional pEC50 = 7.9 7.9 -1 2
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 102034 None 22 Human Functional pEC50 = 7.9 7.9 -1 2
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
168941653 196860 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 264 1 1 1 3.7 CN1CCC=C(c2c[nH]c3c(Cl)c(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
CHEMBL5433583 196860 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 264 1 1 1 3.7 CN1CCC=C(c2c[nH]c3c(Cl)c(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
10401602 123135 None 0 Human Functional pEC50 = 7.0 7.0 -3 3
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 123135 None 0 Human Functional pEC50 = 7.0 7.0 -3 3
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 59260 None 0 Human Functional pEC50 = 6.0 6.0 -6 2
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 59260 None 0 Human Functional pEC50 = 6.0 6.0 -6 2
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 83523 None 0 Human Functional pEC50 = 7.0 7.0 -2 3
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 83523 None 0 Human Functional pEC50 = 7.0 7.0 -2 3
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 183788 None 0 Human Functional pEC50 = 7.0 7.0 -42 3
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 183788 None 0 Human Functional pEC50 = 7.0 7.0 -42 3
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 183788 None 0 Human Functional pEC50 = 7.0 7.0 -42 3
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 192902 None 0 Human Functional pEC50 = 6.0 6.0 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192902 None 0 Human Functional pEC50 = 6.0 6.0 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192902 None 0 Human Functional pEC50 = 6.0 6.0 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183856 None 0 Human Functional pEC50 = 7.0 7.0 -41 3
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 183856 None 0 Human Functional pEC50 = 7.0 7.0 -41 3
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 183856 None 0 Human Functional pEC50 = 7.0 7.0 -41 3
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 77797 None 4 Human Functional pEC50 = 6.0 6.0 -10 3
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 77797 None 4 Human Functional pEC50 = 6.0 6.0 -10 3
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 192902 None 0 Human Functional pEC50 = 6.0 6.0 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5177484 192902 None 0 Human Functional pEC50 = 6.0 6.0 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1ccc(Br)cc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221391 192902 None 0 Human Functional pEC50 = 6.0 6.0 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183856 None 0 Human Functional pEC50 = 7.0 7.0 -41 3
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 183856 None 0 Human Functional pEC50 = 7.0 7.0 -41 3
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 183856 None 0 Human Functional pEC50 = 7.0 7.0 -41 3
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 199963 None 0 Human Functional pEC50 = 6.9 6.9 -4 2
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 199963 None 0 Human Functional pEC50 = 6.9 6.9 -4 2
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 192995 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192995 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192995 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941574 195420 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2c(C3=CCCNC3)n[nH]c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5403370 195420 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2c(C3=CCCNC3)n[nH]c2c1 10.1021/acsmedchemlett.3c00444
168282376 192995 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192995 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192995 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 78331 None 1 Human Functional pEC50 = 6.9 6.9 -5 3
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 78331 None 1 Human Functional pEC50 = 6.9 6.9 -5 3
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 183799 None 0 Human Functional pEC50 = 6.9 6.9 -13 3
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 183799 None 0 Human Functional pEC50 = 6.9 6.9 -13 3
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 183799 None 0 Human Functional pEC50 = 6.9 6.9 -13 3
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 183799 None 0 Human Functional pEC50 = 6.9 6.9 -13 3
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 183799 None 0 Human Functional pEC50 = 6.9 6.9 -13 3
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 183799 None 0 Human Functional pEC50 = 6.9 6.9 -13 3
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 84282 None 4 Human Functional pEC50 = 5.9 5.9 -74 3
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 84282 None 4 Human Functional pEC50 = 5.9 5.9 -74 3
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 138447 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 138447 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 138447 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 102034 None 22 Human Functional pEC50 = 7.9 7.9 -1 2
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 102034 None 22 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
Agonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assayAgonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.2c00716
5202 139 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
Agonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assayAgonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.2c00716
CHEMBL39 139 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
Agonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assayAgonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.2c00716
DB08839 139 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
Agonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assayAgonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs by ONE-Glo reagent based luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jnatprod.2c00716
5 139 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
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 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
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 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
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 None 45 Human Functional pEC50 = 7.9 7.9 -15 26
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
168941477 194997 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 229 2 2 3 1.9 COc1cccc2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5394639 194997 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 229 2 2 3 1.9 COc1cccc2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL4790446 216558 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216558 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216558 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216558 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941556 196480 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 265 1 1 2 3.1 CN1CCC=C(c2n[nH]c3c(Cl)cc(F)cc23)C1 10.1021/acsmedchemlett.3c00444
CHEMBL5424784 196480 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 265 1 1 2 3.1 CN1CCC=C(c2n[nH]c3c(Cl)cc(F)cc23)C1 10.1021/acsmedchemlett.3c00444
1621 2429 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 201656 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 201656 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 192977 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192977 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192977 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192977 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192977 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192977 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138447 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 138447 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 138447 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 102543 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 102543 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 102543 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 None 33 Human Functional pEC50 = 5.9 5.9 -6 2
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 120708 None 0 Human Functional pEC50 = 5.9 5.9 -93 3
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 120708 None 0 Human Functional pEC50 = 5.9 5.9 -93 3
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 120708 None 0 Human Functional pEC50 = 5.9 5.9 -93 3
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 56866 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 56866 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 84872 None 0 Human Functional pEC50 = 6.9 6.9 -87 3
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 84872 None 0 Human Functional pEC50 = 6.9 6.9 -87 3
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 91126 None 0 Human Functional pEC50 = 6.9 6.9 -40 3
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 91126 None 0 Human Functional pEC50 = 6.9 6.9 -40 3
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 192898 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192898 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192898 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192898 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5177718 192898 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 296 1 3 2 3.6 Cc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221369 192898 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 89143 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 89143 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 89143 None 0 Human Functional pEC50 = 6.9 6.9 -47 3
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 207931 None 0 Human Functional pEC50 = 6.9 6.9 -4 3
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 207931 None 0 Human Functional pEC50 = 6.9 6.9 -4 3
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 63324 None 2 Human Functional pEC50 = 6.9 6.9 -7 3
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 63324 None 2 Human Functional pEC50 = 6.9 6.9 -7 3
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 64330 None 3 Human Functional pEC50 = 6.9 6.9 -42 3
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 64330 None 3 Human Functional pEC50 = 6.9 6.9 -42 3
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 94935 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
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 94935 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
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 193005 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 114368 None 3 Human Functional pEC50 = 5.9 5.9 - 1
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 114368 None 3 Human Functional pEC50 = 5.9 5.9 - 1
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 137453 None 0 Human Functional pEC50 = 6.9 6.9 2 3
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 137453 None 0 Human Functional pEC50 = 6.9 6.9 2 3
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 193005 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193005 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 89144 None 0 Human Functional pEC50 = 6.9 6.9 -114 3
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 89144 None 0 Human Functional pEC50 = 6.9 6.9 -114 3
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 89144 None 0 Human Functional pEC50 = 6.9 6.9 -114 3
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 89161 None 0 Human Functional pEC50 = 6.9 6.9 -38 3
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 89161 None 0 Human Functional pEC50 = 6.9 6.9 -38 3
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 89161 None 0 Human Functional pEC50 = 6.9 6.9 -38 3
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 87341 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 87341 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 None 10 Human Functional pEC50 = 7.9 7.9 -1 2
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 120083 None 57 Human Functional pEC50 = 6.9 6.9 -9 9
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 120083 None 57 Human Functional pEC50 = 6.9 6.9 -9 9
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 120083 None 57 Human Functional pEC50 = 6.9 6.9 -9 9
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 8064 None 1 Human Functional pEC50 = 6.9 6.9 -128 2
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 8064 None 1 Human Functional pEC50 = 6.9 6.9 -128 2
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 None 45 Human Functional pEC50 = 6.9 6.9 -15 26
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 201768 None 0 Human Functional pEC50 = 6.9 6.9 -70 3
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 201768 None 0 Human Functional pEC50 = 6.9 6.9 -70 3
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 87341 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 87341 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
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 120720 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
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 120720 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
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 120720 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
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 83531 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
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 83531 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
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 None 19 Human Functional pEC50 = 6.9 6.9 -36 5
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 None 19 Human Functional pEC50 = 6.9 6.9 -36 5
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 None 19 Human Functional pEC50 = 6.9 6.9 -36 5
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 164848 None 0 Human Functional pEC50 = 5.9 5.9 -223 3
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 164848 None 0 Human Functional pEC50 = 5.9 5.9 -223 3
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 202492 None 0 Human Functional pEC50 = 5.9 5.9 -60 3
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 202492 None 0 Human Functional pEC50 = 5.9 5.9 -60 3
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 192946 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192946 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192946 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192946 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192946 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192946 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193139 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193139 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193139 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 190421 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 190421 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 193139 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193139 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193139 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192972 None 0 Human Functional pEC50 = 5.9 5.9 -41 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192972 None 0 Human Functional pEC50 = 5.9 5.9 -41 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192972 None 0 Human Functional pEC50 = 5.9 5.9 -41 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192972 None 0 Human Functional pEC50 = 5.9 5.9 -41 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192972 None 0 Human Functional pEC50 = 5.9 5.9 -41 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192972 None 0 Human Functional pEC50 = 5.9 5.9 -41 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 64330 None 3 Human Functional pEC50 = 6.9 6.9 -42 3
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 64330 None 3 Human Functional pEC50 = 6.9 6.9 -42 3
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 91153 None 0 Human Functional pEC50 = 5.9 5.9 -87 2
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 91153 None 0 Human Functional pEC50 = 5.9 5.9 -87 2
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 56817 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
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 56817 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
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 187737 None 28 Human Functional pEC50 = 6.9 6.9 -95 6
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
CHEMBL4743049 187737 None 28 Human Functional pEC50 = 6.9 6.9 -95 6
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 187737 None 28 Human Functional pEC50 = 6.9 6.9 -95 6
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 193073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 12471 None 5 Human Functional pEC50 = 5.9 5.9 -263 3
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 12471 None 5 Human Functional pEC50 = 5.9 5.9 -263 3
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 12471 None 5 Human Functional pEC50 = 5.9 5.9 -263 3
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 12678 None 15 Human Functional pEC50 = 5.9 5.9 -109 3
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 12678 None 15 Human Functional pEC50 = 5.9 5.9 -109 3
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 12678 None 15 Human Functional pEC50 = 5.9 5.9 -109 3
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 187737 None 28 Human Functional pEC50 = 6.9 6.9 -95 6
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
CHEMBL4743049 187737 None 28 Human Functional pEC50 = 6.9 6.9 -95 6
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 187737 None 28 Human Functional pEC50 = 6.9 6.9 -95 6
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 193052 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193052 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193052 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193052 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193052 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193052 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 202511 None 0 Human Functional pEC50 = 5.8 5.8 -1445 2
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 202511 None 0 Human Functional pEC50 = 5.8 5.8 -1445 2
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 59588 None 2 Human Functional pEC50 = 6.8 6.8 -724 2
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 59588 None 2 Human Functional pEC50 = 6.8 6.8 -724 2
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 193001 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 193001 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 193001 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941768 196057 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 212 1 2 1 2.9 Cc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5416033 196057 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 212 1 2 1 2.9 Cc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
5 139 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 193001 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185474 193001 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 360 1 3 2 4.0 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222039 193001 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 120719 None 0 Human Functional pEC50 = 5.8 5.8 -46 3
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 120719 None 0 Human Functional pEC50 = 5.8 5.8 -46 3
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 120719 None 0 Human Functional pEC50 = 5.8 5.8 -46 3
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 91151 None 0 Human Functional pEC50 = 6.8 6.8 -24 2
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 91151 None 0 Human Functional pEC50 = 6.8 6.8 -24 2
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 12627 None 0 Human Functional pEC50 = 5.8 5.8 -48 3
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 12627 None 0 Human Functional pEC50 = 5.8 5.8 -48 3
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 12627 None 0 Human Functional pEC50 = 5.8 5.8 -48 3
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 216555 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216555 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216555 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216555 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
1621 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
17 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
5761 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
CHEMBL263881 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
DB04829 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
5 139 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 None 45 Human Functional pEC50 = 6.8 6.8 -15 26
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 98073 None 55 Human Functional pEC50 = 6.8 6.8 -1 4
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 98073 None 55 Human Functional pEC50 = 6.8 6.8 -1 4
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 64615 None 16 Human Functional pEC50 = 6.8 6.8 -5 3
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 64615 None 16 Human Functional pEC50 = 6.8 6.8 -5 3
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 202316 None 0 Human Functional pEC50 = 5.8 5.8 -1071 3
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 202316 None 0 Human Functional pEC50 = 5.8 5.8 -1071 3
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 192885 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192885 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192885 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192885 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192885 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192885 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138444 None 0 Human Functional pEC50 = 6.8 6.8 -15 3
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 138444 None 0 Human Functional pEC50 = 6.8 6.8 -15 3
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 138444 None 0 Human Functional pEC50 = 6.8 6.8 -15 3
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 8444 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 8444 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 102457 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 102457 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 102457 None 0 Human Functional pEC50 = 6.8 6.8 4 2
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 192984 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192984 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192984 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192984 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192984 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192984 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193057 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193057 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193057 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 64615 None 16 Human Functional pEC50 = 6.8 6.8 -5 3
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 64615 None 16 Human Functional pEC50 = 6.8 6.8 -5 3
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 192968 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192968 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192968 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193104 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193104 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193104 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 62571 None 7 Human Functional pEC50 = 5.8 5.8 -3 2
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 62571 None 7 Human Functional pEC50 = 5.8 5.8 -3 2
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 130237 None 20 Human Functional pEC50 = 5.8 5.8 -4 3
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 130237 None 20 Human Functional pEC50 = 5.8 5.8 -4 3
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 154505 None 0 Human Functional pEC50 = 5.8 5.8 -7 2
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 154505 None 0 Human Functional pEC50 = 5.8 5.8 -7 2
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 193057 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193057 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193057 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192968 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192968 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192968 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
1621 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
17 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
5761 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
CHEMBL263881 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
DB04829 2429 None 10 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase 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/acsmedchemlett.4c00058
9991444 62652 None 1 Human Functional pEC50 = 7.8 7.8 -4 3
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 62652 None 1 Human Functional pEC50 = 7.8 7.8 -4 3
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 193104 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193104 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193104 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 200824 None 0 Dog Functional pEC50 = 5.8 5.8 - 1
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 200824 None 0 Dog Functional pEC50 = 5.8 5.8 - 1
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 62571 None 7 Human Functional pEC50 = 5.8 5.8 -3 2
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 62571 None 7 Human Functional pEC50 = 5.8 5.8 -3 2
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 130237 None 20 Human Functional pEC50 = 5.8 5.8 -4 3
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 130237 None 20 Human Functional pEC50 = 5.8 5.8 -4 3
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 12463 None 0 Human Functional pEC50 = 5.8 5.8 -70 3
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 12463 None 0 Human Functional pEC50 = 5.8 5.8 -70 3
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 12463 None 0 Human Functional pEC50 = 5.8 5.8 -70 3
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 84721 None 0 Human Functional pEC50 = 5.8 5.8 -38 3
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 84721 None 0 Human Functional pEC50 = 5.8 5.8 -38 3
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 172980 None 0 Human Functional pEC50 = 6.8 6.8 -16 3
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 172980 None 0 Human Functional pEC50 = 6.8 6.8 -16 3
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
168941556 196480 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 265 1 1 2 3.1 CN1CCC=C(c2n[nH]c3c(Cl)cc(F)cc23)C1 10.1021/acsmedchemlett.3c00444
CHEMBL5424784 196480 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 265 1 1 2 3.1 CN1CCC=C(c2n[nH]c3c(Cl)cc(F)cc23)C1 10.1021/acsmedchemlett.3c00444
168288743 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 None 24 Human Functional pEC50 = 6.8 6.8 -17 11
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 138443 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 138443 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 138443 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 120733 None 0 Human Functional pEC50 = 5.8 5.8 -75 2
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 120733 None 0 Human Functional pEC50 = 5.8 5.8 -75 2
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 120733 None 0 Human Functional pEC50 = 5.8 5.8 -75 2
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 137061 None 0 Human Functional pEC50 = 6.8 6.8 -27 3
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 137061 None 0 Human Functional pEC50 = 6.8 6.8 -27 3
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 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5192627 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(OC)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222395 193056 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 45 Human Functional pEC50 = 6.8 6.8 -4 6
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 None 45 Human Functional pEC50 = 6.8 6.8 -4 6
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 None 45 Human Functional pEC50 = 6.8 6.8 -4 6
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 None 45 Human Functional pEC50 = 6.8 6.8 -4 6
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 138443 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 138443 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 138443 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 89133 None 0 Human Functional pEC50 = 5.8 5.8 -151 3
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 89133 None 0 Human Functional pEC50 = 5.8 5.8 -151 3
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 89133 None 0 Human Functional pEC50 = 5.8 5.8 -151 3
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 12441 None 0 Human Functional pEC50 = 6.8 6.8 -32 3
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 12441 None 0 Human Functional pEC50 = 6.8 6.8 -32 3
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 12441 None 0 Human Functional pEC50 = 6.8 6.8 -32 3
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 192095 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 192095 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 78025 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
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 78025 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
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 12705 None 0 Human Functional pEC50 = 5.8 5.8 -117 3
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 12705 None 0 Human Functional pEC50 = 5.8 5.8 -117 3
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 12705 None 0 Human Functional pEC50 = 5.8 5.8 -117 3
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 191302 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 191302 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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
168941766 197177 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 251 1 2 2 2.7 Fc1ccc(Cl)c2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5440436 197177 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 251 1 2 2 2.7 Fc1ccc(Cl)c2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
122442263 138444 None 0 Human Functional pEC50 = 7.8 7.8 -15 3
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 138444 None 0 Human Functional pEC50 = 7.8 7.8 -15 3
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 138444 None 0 Human Functional pEC50 = 7.8 7.8 -15 3
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
168941715 196900 None 0 Human Functional pEC50 = 7.8 7.8 -8 3
Agonist activity at 5-HT2A receptor (unknown origin)Agonist activity at 5-HT2A receptor (unknown origin)
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5434434 196900 None 0 Human Functional pEC50 = 7.8 7.8 -8 3
Agonist activity at 5-HT2A receptor (unknown origin)Agonist activity at 5-HT2A receptor (unknown origin)
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
11160564 63324 None 2 Human Functional pEC50 = 6.8 6.8 -7 3
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 63324 None 2 Human Functional pEC50 = 6.8 6.8 -7 3
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 190421 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 190421 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 84714 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
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 84714 None 0 Human Functional pEC50 = 6.8 6.8 -25 3
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 192900 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192900 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192900 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192900 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192900 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192900 None 0 Human Functional pEC50 = 6.8 6.8 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 85050 None 0 Human Functional pEC50 = 5.8 5.8 -47 3
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 85050 None 0 Human Functional pEC50 = 5.8 5.8 -47 3
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 114366 None 19 Human Functional pEC50 = 7.7 7.7 - 1
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 114366 None 19 Human Functional pEC50 = 7.7 7.7 - 1
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 103095 None 23 Human Functional pEC50 = 7.7 7.7 3 3
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 103095 None 23 Human Functional pEC50 = 7.7 7.7 3 3
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 103095 None 23 Human Functional pEC50 = 7.7 7.7 3 3
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 199247 None 0 Dog Functional pEC50 = 5.8 5.8 - 1
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 199247 None 0 Dog Functional pEC50 = 5.8 5.8 - 1
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 207963 None 0 Human Functional pEC50 = 6.7 6.7 -8 3
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 207963 None 0 Human Functional pEC50 = 6.7 6.7 -8 3
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 120721 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 120721 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 120721 None 0 Human Functional pEC50 = 5.7 5.7 -19 3
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 193042 None 0 Human Functional pEC50 = 5.7 5.7 -4 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 193042 None 0 Human Functional pEC50 = 5.7 5.7 -4 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 193042 None 0 Human Functional pEC50 = 5.7 5.7 -4 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
3568128 193042 None 0 Human Functional pEC50 = 5.7 5.7 -4 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5195443 193042 None 0 Human Functional pEC50 = 5.7 5.7 -4 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222291 193042 None 0 Human Functional pEC50 = 5.7 5.7 -4 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 89098 None 0 Human Functional pEC50 = 5.7 5.7 -70 2
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 89098 None 0 Human Functional pEC50 = 5.7 5.7 -70 2
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 89098 None 0 Human Functional pEC50 = 5.7 5.7 -70 2
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 12657 None 2 Human Functional pEC50 = 5.7 5.7 -190 3
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 12657 None 2 Human Functional pEC50 = 5.7 5.7 -190 3
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 12657 None 2 Human Functional pEC50 = 5.7 5.7 -190 3
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
170453288 196449 None 2 Human Functional pEC50 = 6.7 6.7 -6 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5424175 196449 None 2 Human Functional pEC50 = 6.7 6.7 -6 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
9822580 202976 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 202976 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 178231 None 20 Mouse Functional pEC50 = 7.7 7.7 -5 2
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 178231 None 20 Mouse Functional pEC50 = 7.7 7.7 -5 2
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 103095 None 23 Human Functional pEC50 = 7.7 7.7 3 3
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 103095 None 23 Human Functional pEC50 = 7.7 7.7 3 3
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 103095 None 23 Human Functional pEC50 = 7.7 7.7 3 3
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 178231 None 20 Mouse Functional pEC50 = 7.7 7.7 -5 2
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 178231 None 20 Mouse Functional pEC50 = 7.7 7.7 -5 2
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 62652 None 1 Human Functional pEC50 = 7.7 7.7 -4 3
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 62652 None 1 Human Functional pEC50 = 7.7 7.7 -4 3
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
11291 3220 None 14 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.4c00058
4980 3220 None 14 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.4c00058
CHEMBL65547 3220 None 14 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.4c00058
11658860 2344 None 24 Human Functional pEC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pEC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pEC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pEC50 = 6.7 6.7 -17 11
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 None 24 Human Functional pEC50 = 6.7 6.7 -17 11
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
170453288 196449 None 2 Human Functional pEC50 = 6.7 6.7 -6 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5424175 196449 None 2 Human Functional pEC50 = 6.7 6.7 -6 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 277 1 2 2 2.7 Brc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
168295545 193153 None 0 Human Functional pEC50 = 5.7 5.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193153 None 0 Human Functional pEC50 = 5.7 5.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193153 None 0 Human Functional pEC50 = 5.7 5.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193153 None 0 Human Functional pEC50 = 5.7 5.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193153 None 0 Human Functional pEC50 = 5.7 5.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193153 None 0 Human Functional pEC50 = 5.7 5.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 12524 None 0 Human Functional pEC50 = 5.7 5.7 -52 3
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 12524 None 0 Human Functional pEC50 = 5.7 5.7 -52 3
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 12524 None 0 Human Functional pEC50 = 5.7 5.7 -52 3
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 91133 None 0 Human Functional pEC50 = 6.7 6.7 -16 2
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 91133 None 0 Human Functional pEC50 = 6.7 6.7 -16 2
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 192879 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192879 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192879 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193059 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193059 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193059 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183783 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
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 183783 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
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 183783 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
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 192879 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192879 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192879 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193059 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193059 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193059 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183783 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
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 183783 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
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 183783 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
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 None 26 Human Functional pEC50 = 6.7 6.7 -10 3
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 None 26 Human Functional pEC50 = 6.7 6.7 -10 3
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 None 26 Human Functional pEC50 = 6.7 6.7 -10 3
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 62548 None 2 Human Functional pEC50 = 6.7 6.7 -30 3
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 62548 None 2 Human Functional pEC50 = 6.7 6.7 -30 3
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 64353 None 37 Human Functional pEC50 = 6.7 6.7 -19 3
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 64353 None 37 Human Functional pEC50 = 6.7 6.7 -19 3
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 94910 None 0 Human Functional pEC50 = 6.7 6.7 -25 3
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 94910 None 0 Human Functional pEC50 = 6.7 6.7 -25 3
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 None 24 Human Functional pEC50 = 8.7 8.7 -1 5
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 None 24 Human Functional pEC50 = 8.7 8.7 -1 5
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 None 24 Human Functional pEC50 = 8.7 8.7 -1 5
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
145 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
1832 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
CHEMBL7257 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
DB14010 140 None 16 Human Functional pEC50 = 8.7 8.7 3 12
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acsmedchemlett.3c00566
5 139 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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
14107683 178231 None 20 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acsmedchemlett.4c00058
CHEMBL4648350 178231 None 20 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acsmedchemlett.4c00058
14107683 178231 None 20 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acsmedchemlett.4c00058
CHEMBL4648350 178231 None 20 Human Functional pEC50 = 8.6 8.6 5 2
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2cccc(O)c12 10.1021/acsmedchemlett.4c00058
5 139 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 45 Human Functional pEC50 = 8.6 8.6 -15 26
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 None 50 Human Functional pEC50 = 8.6 8.6 851 2
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 None 50 Human Functional pEC50 = 8.6 8.6 851 2
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 None 50 Human Functional pEC50 = 8.6 8.6 851 2
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 190982 None 8 Human Functional pEC50 = 8.6 8.6 14 2
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 190982 None 8 Human Functional pEC50 = 8.6 8.6 14 2
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
168941564 195265 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5399727 195265 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
50878551 90779 None 28 Human Functional pEC50 = 8.6 8.6 -1 3
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 90779 None 28 Human Functional pEC50 = 8.6 8.6 -1 3
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 188682 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 188682 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 188682 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 138441 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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 138441 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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 138441 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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
85542158 195546 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at 5-HT2A receptor (unknown origin)Agonist activity at 5-HT2A receptor (unknown origin)
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at 5-HT2A receptor (unknown origin)Agonist activity at 5-HT2A receptor (unknown origin)
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at 5-HT2A receptor (unknown origin)Agonist activity at 5-HT2A receptor (unknown origin)
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
122442263 138444 None 0 Human Functional pEC50 = 6.7 6.7 -15 3
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 138444 None 0 Human Functional pEC50 = 6.7 6.7 -15 3
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 138444 None 0 Human Functional pEC50 = 6.7 6.7 -15 3
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 56867 None 0 Human Functional pEC50 = 5.7 5.7 -10 3
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 56867 None 0 Human Functional pEC50 = 5.7 5.7 -10 3
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 91143 None 0 Human Functional pEC50 = 6.7 6.7 -7 2
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 91143 None 0 Human Functional pEC50 = 6.7 6.7 -7 2
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 193122 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193122 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193122 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192901 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192901 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192901 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193132 None 2 Human Functional pEC50 = 6.7 6.7 9 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193132 None 2 Human Functional pEC50 = 6.7 6.7 9 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193132 None 2 Human Functional pEC50 = 6.7 6.7 9 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 205867 None 7 Human Functional pEC50 = 6.7 6.7 1 2
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 205867 None 7 Human Functional pEC50 = 6.7 6.7 1 2
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 192901 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192901 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192901 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193122 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193122 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193122 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193132 None 2 Human Functional pEC50 = 6.7 6.7 9 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193132 None 2 Human Functional pEC50 = 6.7 6.7 9 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193132 None 2 Human Functional pEC50 = 6.7 6.7 9 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 89094 None 0 Human Functional pEC50 = 5.7 5.7 -51 3
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 89094 None 0 Human Functional pEC50 = 5.7 5.7 -51 3
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 89094 None 0 Human Functional pEC50 = 5.7 5.7 -51 3
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 114364 None 42 Human Functional pEC50 = 6.7 6.7 - 1
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 114364 None 42 Human Functional pEC50 = 6.7 6.7 - 1
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 89126 None 0 Human Functional pEC50 = 7.7 7.7 -9 2
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 89126 None 0 Human Functional pEC50 = 7.7 7.7 -9 2
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 89126 None 0 Human Functional pEC50 = 7.7 7.7 -9 2
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 138441 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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 138441 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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 138441 None 0 Human Functional pEC50 = 7.7 7.7 -4 3
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
168941519 195345 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 231 1 1 2 2.4 CN1CCC=C(c2n[nH]c3cc(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
CHEMBL5401711 195345 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 231 1 1 2 2.4 CN1CCC=C(c2n[nH]c3cc(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
27559 205867 None 7 Human Functional pEC50 = 6.7 6.7 1 2
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 205867 None 7 Human Functional pEC50 = 6.7 6.7 1 2
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 138438 None 0 Human Functional pEC50 = 6.7 6.7 -13 3
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 138438 None 0 Human Functional pEC50 = 6.7 6.7 -13 3
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 138438 None 0 Human Functional pEC50 = 6.7 6.7 -13 3
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 183865 None 0 Human Functional pEC50 = 6.7 6.7 -21 3
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 183865 None 0 Human Functional pEC50 = 6.7 6.7 -21 3
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 183865 None 0 Human Functional pEC50 = 6.7 6.7 -21 3
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 183865 None 0 Human Functional pEC50 = 6.7 6.7 -21 3
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 183865 None 0 Human Functional pEC50 = 6.7 6.7 -21 3
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 183865 None 0 Human Functional pEC50 = 6.7 6.7 -21 3
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 138438 None 0 Human Functional pEC50 = 6.7 6.7 -13 3
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 138438 None 0 Human Functional pEC50 = 6.7 6.7 -13 3
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 138438 None 0 Human Functional pEC50 = 6.7 6.7 -13 3
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 193145 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193145 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193145 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 12466 None 0 Human Functional pEC50 = 5.7 5.7 -83 3
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 12466 None 0 Human Functional pEC50 = 5.7 5.7 -83 3
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 12466 None 0 Human Functional pEC50 = 5.7 5.7 -83 3
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 193145 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193145 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193145 None 0 Human Functional pEC50 = 6.7 6.7 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
22241625 196520 None 0 Human Functional pEC50 = 5.7 5.7 -63 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
CHEMBL5425772 196520 None 0 Human Functional pEC50 = 5.7 5.7 -63 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
146025688 183800 None 0 Human Functional pEC50 = 5.7 5.7 -81 3
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 183800 None 0 Human Functional pEC50 = 5.7 5.7 -81 3
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 183800 None 0 Human Functional pEC50 = 5.7 5.7 -81 3
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
168941768 196057 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 212 1 2 1 2.9 Cc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5416033 196057 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 212 1 2 1 2.9 Cc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
24826867 91129 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
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 91129 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
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 183821 None 0 Human Functional pEC50 = 7.7 7.7 -12 3
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 183821 None 0 Human Functional pEC50 = 7.7 7.7 -12 3
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 183821 None 0 Human Functional pEC50 = 7.7 7.7 -12 3
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
11291 3220 None 14 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.4c00058
4980 3220 None 14 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.4c00058
CHEMBL65547 3220 None 14 Human Functional pEC50 = 7.7 7.7 -2 4
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1c(O)ccc2)C 10.1021/acsmedchemlett.4c00058
10472780 63303 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 63303 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 None 18 Human Functional pEC50 = 7.7 7.7 1 15
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 183821 None 0 Human Functional pEC50 = 7.7 7.7 -12 3
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 183821 None 0 Human Functional pEC50 = 7.7 7.7 -12 3
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 183821 None 0 Human Functional pEC50 = 7.7 7.7 -12 3
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 136489 None 0 Human Functional pEC50 = 6.7 6.7 -43 2
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 136489 None 0 Human Functional pEC50 = 6.7 6.7 -43 2
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 62548 None 2 Human Functional pEC50 = 6.7 6.7 -30 3
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 62548 None 2 Human Functional pEC50 = 6.7 6.7 -30 3
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 77762 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 77762 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
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 202196 None 6 Human Functional pEC50 = 5.7 5.7 -87 2
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 202196 None 6 Human Functional pEC50 = 5.7 5.7 -87 2
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
22241625 196520 None 0 Human Functional pEC50 = 5.7 5.7 -63 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
CHEMBL5425772 196520 None 0 Human Functional pEC50 = 5.7 5.7 -63 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 205 3 2 3 1.4 CN(C)CCc1n[nH]c2ccc(O)cc12 10.1021/acsmedchemlett.3c00566
146025688 183800 None 0 Human Functional pEC50 = 5.7 5.7 -81 3
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 183800 None 0 Human Functional pEC50 = 5.7 5.7 -81 3
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 183800 None 0 Human Functional pEC50 = 5.7 5.7 -81 3
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 192923 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192923 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192923 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192923 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192923 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192923 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193023 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 193023 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 193023 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193023 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5196522 193023 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222172 193023 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
85542158 195546 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
27559 205867 None 7 Human Functional pEC50 = 7.6 7.6 1 2
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 205867 None 7 Human Functional pEC50 = 7.6 7.6 1 2
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 190525 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 190525 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192521 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 192521 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 103095 None 23 Human Functional pEC50 = 7.6 7.6 3 3
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 103095 None 23 Human Functional pEC50 = 7.6 7.6 3 3
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 103095 None 23 Human Functional pEC50 = 7.6 7.6 3 3
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 205867 None 7 Human Functional pEC50 = 7.6 7.6 1 2
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 205867 None 7 Human Functional pEC50 = 7.6 7.6 1 2
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 190525 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 190525 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192521 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 192521 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 56814 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
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 56814 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
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
85542158 195546 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 5.6 5.6 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
146025685 183765 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 183765 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 183765 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 138429 None 0 Human Functional pEC50 = 5.6 5.6 -20 3
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 138429 None 0 Human Functional pEC50 = 5.6 5.6 -20 3
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 138429 None 0 Human Functional pEC50 = 5.6 5.6 -20 3
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 138431 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 138431 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 138431 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 183765 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 183765 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 183765 None 0 Human Functional pEC50 = 5.6 5.6 -19 2
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 138429 None 0 Human Functional pEC50 = 5.6 5.6 -20 3
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 138429 None 0 Human Functional pEC50 = 5.6 5.6 -20 3
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 138429 None 0 Human Functional pEC50 = 5.6 5.6 -20 3
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 56813 None 0 Human Functional pEC50 = 5.6 5.6 -436 3
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 56813 None 0 Human Functional pEC50 = 5.6 5.6 -436 3
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 12550 None 0 Human Functional pEC50 = 6.6 6.6 -47 3
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 12550 None 0 Human Functional pEC50 = 6.6 6.6 -47 3
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 12550 None 0 Human Functional pEC50 = 6.6 6.6 -47 3
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 138431 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 138431 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 138431 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 202441 None 0 Human Functional pEC50 = 6.6 6.6 -2344 3
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 202441 None 0 Human Functional pEC50 = 6.6 6.6 -2344 3
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 163774 None 0 Human Functional pEC50 = 6.6 6.6 -204 3
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 163774 None 0 Human Functional pEC50 = 6.6 6.6 -204 3
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 192989 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192989 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192989 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192989 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192989 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192989 None 0 Human Functional pEC50 = 6.6 6.6 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 12566 None 0 Human Functional pEC50 = 5.6 5.6 -199 3
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 12566 None 0 Human Functional pEC50 = 5.6 5.6 -199 3
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 12566 None 0 Human Functional pEC50 = 5.6 5.6 -199 3
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 87344 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
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 87344 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
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
168941461 197064 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 265 1 1 2 3.1 CN1CCC=C(c2n[nH]c3c(Cl)ccc(F)c23)C1 10.1021/acsmedchemlett.3c00444
CHEMBL5437921 197064 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 265 1 1 2 3.1 CN1CCC=C(c2n[nH]c3c(Cl)ccc(F)c23)C1 10.1021/acsmedchemlett.3c00444
11291 3220 None 14 Human Functional pEC50 = 7.6 7.6 -2 4
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 None 14 Human Functional pEC50 = 7.6 7.6 -2 4
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 None 14 Human Functional pEC50 = 7.6 7.6 -2 4
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 87341 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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 87341 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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 87344 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
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 87344 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
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 63000 None 2 Human Functional pEC50 = 5.6 5.6 -9 2
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 63000 None 2 Human Functional pEC50 = 5.6 5.6 -9 2
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 192932 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192932 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192932 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 116863 None 60 Human Functional pEC50 = 5.6 5.6 - 1
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 116863 None 60 Human Functional pEC50 = 5.6 5.6 - 1
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 87341 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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 87341 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
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 192932 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192932 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192932 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216549 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 114370 None 2 Human Functional pEC50 = 6.6 6.6 - 1
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 114370 None 2 Human Functional pEC50 = 6.6 6.6 - 1
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 12710 None 0 Human Functional pEC50 = 6.6 6.6 -74 3
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 12710 None 0 Human Functional pEC50 = 6.6 6.6 -74 3
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 12710 None 0 Human Functional pEC50 = 6.6 6.6 -74 3
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 216549 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 201822 None 0 Human Functional pEC50 = 6.6 6.6 -15 3
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 201822 None 0 Human Functional pEC50 = 6.6 6.6 -15 3
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 114369 None 1 Human Functional pEC50 = 6.6 6.6 - 1
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 114369 None 1 Human Functional pEC50 = 6.6 6.6 - 1
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 78214 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 78214 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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
5 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
5202 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
CHEMBL39 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
DB08839 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
172445373 195170 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs in presence of serotonin by ONE-Glo reagent based luciferase assayAgonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs in presence of serotonin by ONE-Glo reagent based luciferase assay
ChEMBL 244 1 3 3 1.7 CC1=N[C@H](C(=O)O)Cc2c[nH]c3c(O)ccc1c23 10.1021/acs.jnatprod.2c00716
CHEMBL5398022 195170 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs in presence of serotonin by ONE-Glo reagent based luciferase assayAgonist activity at N-terminal HA-tagged human 5HT2A receptor transfected in CHO-K1 cells co-expressing C-terminal EYFP measured for 5.5 hrs in presence of serotonin by ONE-Glo reagent based luciferase assay
ChEMBL 244 1 3 3 1.7 CC1=N[C@H](C(=O)O)Cc2c[nH]c3c(O)ccc1c23 10.1021/acs.jnatprod.2c00716
23652278 62651 None 11 Human Functional pEC50 = 6.6 6.6 -16 3
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 62651 None 11 Human Functional pEC50 = 6.6 6.6 -16 3
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 94912 None 1 Human Functional pEC50 = 6.6 6.6 -6 3
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 94912 None 1 Human Functional pEC50 = 6.6 6.6 -6 3
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 123499 None 6 Human Functional pEC50 = 6.6 6.6 -1 3
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 123499 None 6 Human Functional pEC50 = 6.6 6.6 -1 3
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 192983 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192983 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192983 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 164150 None 0 Human Functional pEC50 = 5.6 5.6 -204 3
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 164150 None 0 Human Functional pEC50 = 5.6 5.6 -204 3
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 63000 None 2 Human Functional pEC50 = 5.6 5.6 -9 2
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 63000 None 2 Human Functional pEC50 = 5.6 5.6 -9 2
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 19058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 19058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 19058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 19058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 19058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 19058 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192983 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5183950 192983 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 326 3 2 3 3.6 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221924 192983 None 0 Human Functional pEC50 = 6.6 6.6 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 200111 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 200111 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 183772 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183772 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183772 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 None 24 Human Functional pEC50 = 6.6 6.6 -17 11
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 183730 None 0 Human Functional pEC50 = 5.6 5.6 -177 3
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 183730 None 0 Human Functional pEC50 = 5.6 5.6 -177 3
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 183730 None 0 Human Functional pEC50 = 5.6 5.6 -177 3
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 192903 None 0 Human Functional pEC50 = 7.6 7.6 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192903 None 0 Human Functional pEC50 = 7.6 7.6 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192903 None 0 Human Functional pEC50 = 7.6 7.6 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192903 None 0 Human Functional pEC50 = 7.6 7.6 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192903 None 0 Human Functional pEC50 = 7.6 7.6 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192903 None 0 Human Functional pEC50 = 7.6 7.6 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 19 Human Functional pEC50 = 7.6 7.6 -36 5
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 None 19 Human Functional pEC50 = 7.6 7.6 -36 5
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 None 19 Human Functional pEC50 = 7.6 7.6 -36 5
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 183772 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183772 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 183772 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 64353 None 37 Human Functional pEC50 = 6.6 6.6 -19 3
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 64353 None 37 Human Functional pEC50 = 6.6 6.6 -19 3
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 216557 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216557 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183730 None 0 Human Functional pEC50 = 5.6 5.6 -177 3
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 183730 None 0 Human Functional pEC50 = 5.6 5.6 -177 3
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 183730 None 0 Human Functional pEC50 = 5.6 5.6 -177 3
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 216557 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216557 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 56863 None 0 Human Functional pEC50 = 5.6 5.6 -27 3
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 56863 None 0 Human Functional pEC50 = 5.6 5.6 -27 3
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 62651 None 11 Human Functional pEC50 = 6.6 6.6 -16 3
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 62651 None 11 Human Functional pEC50 = 6.6 6.6 -16 3
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 56822 None 0 Human Functional pEC50 = 5.6 5.6 -32 3
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 56822 None 0 Human Functional pEC50 = 5.6 5.6 -32 3
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 193125 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193125 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193125 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 120853 None 0 Human Functional pEC50 = 6.6 6.6 -46 2
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 120853 None 0 Human Functional pEC50 = 6.6 6.6 -46 2
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 193125 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193125 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193125 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 None 19 Human Functional pEC50 = 7.6 7.6 -36 5
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 None 19 Human Functional pEC50 = 7.6 7.6 -36 5
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 None 19 Human Functional pEC50 = 7.6 7.6 -36 5
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 90779 None 28 Human Functional pEC50 = 7.6 7.6 -1 3
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 90779 None 28 Human Functional pEC50 = 7.6 7.6 -1 3
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 102544 None 0 Human Functional pEC50 = 7.6 7.6 1 7
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 102544 None 0 Human Functional pEC50 = 7.6 7.6 1 7
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 102544 None 0 Human Functional pEC50 = 7.6 7.6 1 7
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 193116 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5205429 193116 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222746 193116 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193054 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193054 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193054 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193116 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5205429 193116 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 316 1 3 2 3.9 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(F)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222746 193116 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193054 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193054 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193054 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
5 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
5202 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
CHEMBL39 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
DB08839 139 None 45 Human Functional pEC50 = 7.6 7.6 -15 26
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acsmedchemlett.4c00058
20976025 141174 None 29 Human Functional pEC50 = 7.6 7.6 - 1
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 141174 None 29 Human Functional pEC50 = 7.6 7.6 - 1
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 192958 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192958 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192958 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192958 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192958 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192958 None 0 Human Functional pEC50 = 6.6 6.6 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193131 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193131 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193131 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193131 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193131 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193131 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
172469352 197023 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5437030 197023 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
168295538 193148 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193148 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193148 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193148 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193148 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193148 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 164549 None 0 Human Functional pEC50 = 5.5 5.5 -85 3
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 164549 None 0 Human Functional pEC50 = 5.5 5.5 -85 3
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
172469352 197023 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5437030 197023 None 0 Human Functional pEC50 = 5.5 5.5 -288 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 214 1 3 3 1.5 Nc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
16115652 83524 None 0 Human Functional pEC50 = 6.5 6.5 -26 3
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 83524 None 0 Human Functional pEC50 = 6.5 6.5 -26 3
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 None 45 Human Functional pEC50 = 6.5 6.5 -4 6
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 102553 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 102553 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 102553 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 183721 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 183721 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 183721 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 216556 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216556 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183721 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 183721 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 183721 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 183796 None 0 Human Functional pEC50 = 6.5 6.5 -47 3
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 183796 None 0 Human Functional pEC50 = 6.5 6.5 -47 3
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 183796 None 0 Human Functional pEC50 = 6.5 6.5 -47 3
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 216556 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216556 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183796 None 0 Human Functional pEC50 = 6.5 6.5 -47 3
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 183796 None 0 Human Functional pEC50 = 6.5 6.5 -47 3
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 183796 None 0 Human Functional pEC50 = 6.5 6.5 -47 3
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 120707 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
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 120707 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
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 120707 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
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
168941678 195526 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 242 2 1 2 2.9 COc1cccc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5405349 195526 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 242 2 1 2 2.9 COc1cccc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
53325937 56821 None 0 Human Functional pEC50 = 8.5 8.5 7 3
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 56821 None 0 Human Functional pEC50 = 8.5 8.5 7 3
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 192288 None 0 Human Functional pEC50 = 8.5 8.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192288 None 0 Human Functional pEC50 = 8.5 8.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
168293874 192288 None 0 Human Functional pEC50 = 8.5 8.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192288 None 0 Human Functional pEC50 = 8.5 8.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941548 196083 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 233 1 2 2 2.6 Clc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5416604 196083 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 233 1 2 2 2.6 Clc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
168273228 192908 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192908 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192908 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941728 197186 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 228 2 2 2 2.6 COc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5440705 197186 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 228 2 2 2 2.6 COc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
168273228 192908 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192908 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192908 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 64904 None 0 Human Functional pEC50 = 7.5 7.5 -6 3
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 64904 None 0 Human Functional pEC50 = 7.5 7.5 -6 3
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 186162 None 8 Human Functional pEC50 = 7.5 7.5 - 1
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 186162 None 8 Human Functional pEC50 = 7.5 7.5 - 1
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 191385 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 191385 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 None 24 Human Functional pEC50 = 6.5 6.5 -17 11
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 None 24 Human Functional pEC50 = 6.5 6.5 -17 11
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 None 24 Human Functional pEC50 = 6.5 6.5 -17 11
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 None 24 Human Functional pEC50 = 6.5 6.5 -17 11
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 None 24 Human Functional pEC50 = 6.5 6.5 -17 11
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 192922 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192922 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192922 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216551 None 26 Human Functional pEC50 = 6.5 6.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216551 None 26 Human Functional pEC50 = 6.5 6.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 74484 None 0 Human Functional pEC50 = 5.5 5.5 -169 3
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 74484 None 0 Human Functional pEC50 = 5.5 5.5 -169 3
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 74484 None 0 Human Functional pEC50 = 5.5 5.5 -169 3
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 89141 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 89141 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 89141 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 216551 None 26 Human Functional pEC50 = 6.5 6.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216551 None 26 Human Functional pEC50 = 6.5 6.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 200279 None 0 Human Functional pEC50 = 6.5 6.5 -30 3
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 200279 None 0 Human Functional pEC50 = 6.5 6.5 -30 3
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 154947 None 0 Human Functional pEC50 = 7.5 7.5 -5 3
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 154947 None 0 Human Functional pEC50 = 7.5 7.5 -5 3
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 193097 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193097 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193097 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 94913 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 94913 None 0 Human Functional pEC50 = 6.5 6.5 -15 3
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 193097 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193097 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193097 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 187296 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
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 187296 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
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 56820 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 56820 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 72249 None 0 Human Functional pEC50 = 7.5 7.5 19 2
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 72249 None 0 Human Functional pEC50 = 7.5 7.5 19 2
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
85542158 195546 None 0 Human Functional pEC50 = 5.5 5.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 5.5 5.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 5.5 5.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
172444062 195485 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
CHEMBL5404610 195485 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
168941654 195567 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
CHEMBL5406172 195567 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
85542158 195546 None 0 Human Functional pEC50 = 5.5 5.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5405688 195546 None 0 Human Functional pEC50 = 5.5 5.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5439312 195546 None 0 Human Functional pEC50 = 5.5 5.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 219 4 1 3 1.7 COc1ccc2[nH]nc(CCN(C)C)c2c1 10.1021/acsmedchemlett.3c00566
168941654 195567 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
CHEMBL5406172 195567 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 199 1 2 2 1.9 C1=C(c2n[nH]c3ccccc23)CNCC1 10.1021/acsmedchemlett.3c00566
172444062 195485 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
CHEMBL5404610 195485 None 0 Human Functional pEC50 = 6.5 6.5 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 1 3 2.0 Cn1nc(C2=CCCNC2)c2ccccc21 10.1021/acsmedchemlett.3c00566
16115511 84871 None 0 Human Functional pEC50 = 5.5 5.5 -72 3
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 84871 None 0 Human Functional pEC50 = 5.5 5.5 -72 3
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 12706 None 0 Human Functional pEC50 = 6.5 6.5 -25 3
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 12706 None 0 Human Functional pEC50 = 6.5 6.5 -25 3
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 12706 None 0 Human Functional pEC50 = 6.5 6.5 -25 3
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 216559 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216559 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216559 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216559 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192993 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192993 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192993 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
168282202 192993 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5185430 192993 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1c(Cl)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5221991 192993 None 0 Human Functional pEC50 = 6.5 6.5 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 61474 None 27 Dog Functional pEC50 = 5.5 5.5 -316 9
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 61474 None 27 Dog Functional pEC50 = 5.5 5.5 -316 9
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 193068 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193068 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193068 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193074 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193074 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193074 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193068 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193068 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193068 None 0 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193074 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193074 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193074 None 0 Human Functional pEC50 = 6.5 6.5 3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 70324 None 12 Human Functional pEC50 = 5.5 5.5 -46 3
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
10624.0 70324 None 12 Human Functional pEC50 = 5.5 5.5 -46 3
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 70324 None 12 Human Functional pEC50 = 5.5 5.5 -46 3
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 70324 None 12 Human Functional pEC50 = 5.5 5.5 -46 3
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
DB11664 70324 None 12 Human Functional pEC50 = 5.5 5.5 -46 3
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 59675 None 0 Human Functional pEC50 = 6.5 6.5 -1513 2
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 59675 None 0 Human Functional pEC50 = 6.5 6.5 -1513 2
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 12488 None 0 Human Functional pEC50 = 6.5 6.5 -31 3
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 12488 None 0 Human Functional pEC50 = 6.5 6.5 -31 3
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 12488 None 0 Human Functional pEC50 = 6.5 6.5 -31 3
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 193138 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193138 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193138 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183798 None 0 Human Functional pEC50 = 6.5 6.5 -38 3
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 183798 None 0 Human Functional pEC50 = 6.5 6.5 -38 3
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 183798 None 0 Human Functional pEC50 = 6.5 6.5 -38 3
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 193138 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193138 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193138 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183798 None 0 Human Functional pEC50 = 6.5 6.5 -38 3
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 183798 None 0 Human Functional pEC50 = 6.5 6.5 -38 3
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 183798 None 0 Human Functional pEC50 = 6.5 6.5 -38 3
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
172456366 196390 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 274 2 2 1 4.2 C1=C(c2c[nH]c3cccc(-c4ccccc4)c23)CNCC1 10.1021/acsmedchemlett.3c00444
CHEMBL5422786 196390 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 274 2 2 1 4.2 C1=C(c2c[nH]c3cccc(-c4ccccc4)c23)CNCC1 10.1021/acsmedchemlett.3c00444
92042921 120734 None 0 Human Functional pEC50 = 6.5 6.5 -104 2
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 120734 None 0 Human Functional pEC50 = 6.5 6.5 -104 2
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 120734 None 0 Human Functional pEC50 = 6.5 6.5 -104 2
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 12565 None 0 Human Functional pEC50 = 6.4 6.4 -51 3
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 12565 None 0 Human Functional pEC50 = 6.4 6.4 -51 3
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 12565 None 0 Human Functional pEC50 = 6.4 6.4 -51 3
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 138434 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 138434 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 138434 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 193007 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 193007 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 193007 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192919 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192919 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192919 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193007 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5186011 193007 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 294 1 2 1 4.2 Cc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222066 193007 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138434 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 138434 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 138434 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 192919 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192919 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192919 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 207910 None 0 Human Functional pEC50 = 6.4 6.4 -51 3
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 207910 None 0 Human Functional pEC50 = 6.4 6.4 -51 3
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 91136 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
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 91136 None 0 Human Functional pEC50 = 7.4 7.4 -9 3
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 183768 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
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 183768 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
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 183768 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
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 183768 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
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 183768 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
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 183768 None 0 Human Functional pEC50 = 7.4 7.4 -22 3
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 164108 None 0 Human Functional pEC50 = 7.4 7.4 -194 3
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 164108 None 0 Human Functional pEC50 = 7.4 7.4 -194 3
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 138216 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 138216 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 192970 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192970 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192970 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192970 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192970 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192970 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
172448061 195947 None 0 Human Functional pEC50 = 6.4 6.4 -39 2
Agonist activity at N-terminal HA-tagged human 5HT2A receptorAgonist activity at N-terminal HA-tagged human 5HT2A receptor
ChEMBL 233 5 2 3 2.2 NC[C@@H]1C[C@@H]1c1cc(O)ccc1OCC1CC1 10.1016/j.bmcl.2024.129654
CHEMBL5413973 195947 None 0 Human Functional pEC50 = 6.4 6.4 -39 2
Agonist activity at N-terminal HA-tagged human 5HT2A receptorAgonist activity at N-terminal HA-tagged human 5HT2A receptor
ChEMBL 233 5 2 3 2.2 NC[C@@H]1C[C@@H]1c1cc(O)ccc1OCC1CC1 10.1016/j.bmcl.2024.129654
16115644 137047 None 0 Human Functional pEC50 = 6.4 6.4 -21 3
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 137047 None 0 Human Functional pEC50 = 6.4 6.4 -21 3
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 120731 None 0 Human Functional pEC50 = 6.4 6.4 -89 2
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 120731 None 0 Human Functional pEC50 = 6.4 6.4 -89 2
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 120731 None 0 Human Functional pEC50 = 6.4 6.4 -89 2
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 207980 None 0 Human Functional pEC50 = 6.4 6.4 -9 3
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 207980 None 0 Human Functional pEC50 = 6.4 6.4 -9 3
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 138444 None 0 Human Functional pEC50 = 7.4 7.4 -15 3
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 138444 None 0 Human Functional pEC50 = 7.4 7.4 -15 3
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 138444 None 0 Human Functional pEC50 = 7.4 7.4 -15 3
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 114363 None 7 Human Functional pEC50 = 7.4 7.4 - 1
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 114363 None 7 Human Functional pEC50 = 7.4 7.4 - 1
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 91132 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 91132 None 0 Human Functional pEC50 = 6.4 6.4 -17 2
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -12 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -12 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -12 3
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 183833 None 0 Human Functional pEC50 = 6.4 6.4 -38 2
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 183833 None 0 Human Functional pEC50 = 6.4 6.4 -38 2
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 183833 None 0 Human Functional pEC50 = 6.4 6.4 -38 2
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 192967 None 0 Human Functional pEC50 = 6.4 6.4 10 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192967 None 0 Human Functional pEC50 = 6.4 6.4 10 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192967 None 0 Human Functional pEC50 = 6.4 6.4 10 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192975 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192975 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192975 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192975 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192975 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192975 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192967 None 0 Human Functional pEC50 = 6.4 6.4 10 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192967 None 0 Human Functional pEC50 = 6.4 6.4 10 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192967 None 0 Human Functional pEC50 = 6.4 6.4 10 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183833 None 0 Human Functional pEC50 = 6.4 6.4 -38 2
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 183833 None 0 Human Functional pEC50 = 6.4 6.4 -38 2
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 183833 None 0 Human Functional pEC50 = 6.4 6.4 -38 2
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -12 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -12 3
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 183801 None 0 Human Functional pEC50 = 6.4 6.4 -12 3
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 192966 None 0 Human Functional pEC50 = 6.4 6.4 19 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192966 None 0 Human Functional pEC50 = 6.4 6.4 19 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192966 None 0 Human Functional pEC50 = 6.4 6.4 19 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192966 None 0 Human Functional pEC50 = 6.4 6.4 19 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192966 None 0 Human Functional pEC50 = 6.4 6.4 19 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192966 None 0 Human Functional pEC50 = 6.4 6.4 19 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 19053 None 44 Human Functional pEC50 = 8.4 8.4 - 1
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 19053 None 44 Human Functional pEC50 = 8.4 8.4 - 1
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 None 14 Human Functional pEC50 = 8.4 8.4 -2 4
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 None 14 Human Functional pEC50 = 8.4 8.4 -2 4
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 None 14 Human Functional pEC50 = 8.4 8.4 -2 4
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 None 14 Human Functional pEC50 = 8.4 8.4 -2 4
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 None 14 Human Functional pEC50 = 8.4 8.4 -2 4
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 None 14 Human Functional pEC50 = 8.4 8.4 -2 4
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 140647 None 46 Human Functional pEC50 = 8.3 8.3 - 1
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 140647 None 46 Human Functional pEC50 = 8.3 8.3 - 1
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 56862 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 56862 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 78125 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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 78125 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
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
172445742 197396 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assayAgonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assay
ChEMBL 239 0 1 3 2.6 Cc1cc2nc3c(nc2cc1C)[C@@H]1CCC(C3)N1 10.1021/acs.jmedchem.3c01059
CHEMBL5394878 197396 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assayAgonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assay
ChEMBL 239 0 1 3 2.6 Cc1cc2nc3c(nc2cc1C)[C@@H]1CCC(C3)N1 10.1021/acs.jmedchem.3c01059
CHEMBL5498883 197396 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assayAgonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assay
ChEMBL 239 0 1 3 2.6 Cc1cc2nc3c(nc2cc1C)[C@@H]1CCC(C3)N1 10.1021/acs.jmedchem.3c01059
166 3359 None 19 Human Functional pEC50 = 6.4 6.4 -36 5
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 None 19 Human Functional pEC50 = 6.4 6.4 -36 5
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 None 19 Human Functional pEC50 = 6.4 6.4 -36 5
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 120714 None 0 Human Functional pEC50 = 5.4 5.4 -43 3
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 120714 None 0 Human Functional pEC50 = 5.4 5.4 -43 3
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 120714 None 0 Human Functional pEC50 = 5.4 5.4 -43 3
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 192907 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192907 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192907 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192907 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192907 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192907 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192942 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192942 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192942 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192942 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192942 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192942 None 0 Human Functional pEC50 = 6.4 6.4 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 200008 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 200008 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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
164513426 195281 None 0 Human Functional pEC50 = 7.4 7.4 4 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 2 2 2.2 C[C@@H]1C=C(c2c[nH]c3ncccc23)CNC1 10.1021/acsmedchemlett.3c00566
CHEMBL5399968 195281 None 0 Human Functional pEC50 = 7.4 7.4 4 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 213 1 2 2 2.2 C[C@@H]1C=C(c2c[nH]c3ncccc23)CNC1 10.1021/acsmedchemlett.3c00566
44412403 77827 None 0 Human Functional pEC50 = 6.4 6.4 -7 3
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 77827 None 0 Human Functional pEC50 = 6.4 6.4 -7 3
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 63505 None 0 Human Functional pEC50 = 7.4 7.4 -10 3
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 63505 None 0 Human Functional pEC50 = 7.4 7.4 -10 3
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 138446 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 138446 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 138446 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 None 33 Human Functional pEC50 = 6.4 6.4 -6 2
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 138446 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 138446 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 138446 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 207391 None 0 Human Functional pEC50 = 6.4 6.4 -19 3
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 207391 None 0 Human Functional pEC50 = 6.4 6.4 -19 3
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 138432 None 0 Human Functional pEC50 = 6.4 6.4 -33 3
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 138432 None 0 Human Functional pEC50 = 6.4 6.4 -33 3
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 138432 None 0 Human Functional pEC50 = 6.4 6.4 -33 3
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 12654 None 1 Human Functional pEC50 = 6.4 6.4 -131 3
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 12654 None 1 Human Functional pEC50 = 6.4 6.4 -131 3
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 12654 None 1 Human Functional pEC50 = 6.4 6.4 -131 3
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 138432 None 0 Human Functional pEC50 = 6.4 6.4 -33 3
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 138432 None 0 Human Functional pEC50 = 6.4 6.4 -33 3
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 138432 None 0 Human Functional pEC50 = 6.4 6.4 -33 3
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 121856 None 1 Human Functional pEC50 = 7.4 7.4 - 1
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 121856 None 1 Human Functional pEC50 = 7.4 7.4 - 1
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 75818 None 43 Human Functional pEC50 = 7.4 7.4 89 2
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 75818 None 43 Human Functional pEC50 = 7.4 7.4 89 2
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 75818 None 43 Human Functional pEC50 = 7.4 7.4 89 2
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 8063 None 22 Human Functional pEC50 = 6.4 6.4 -190 2
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 8063 None 22 Human Functional pEC50 = 6.4 6.4 -190 2
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 12518 None 0 Human Functional pEC50 = 5.4 5.4 -58 3
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 12518 None 0 Human Functional pEC50 = 5.4 5.4 -58 3
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 12518 None 0 Human Functional pEC50 = 5.4 5.4 -58 3
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 84928 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 84928 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
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 191302 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 191302 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 192963 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192963 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192963 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183787 None 0 Human Functional pEC50 = 6.3 6.3 -38 3
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 183787 None 0 Human Functional pEC50 = 6.3 6.3 -38 3
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 183787 None 0 Human Functional pEC50 = 6.3 6.3 -38 3
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 183787 None 0 Human Functional pEC50 = 6.3 6.3 -38 3
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 183787 None 0 Human Functional pEC50 = 6.3 6.3 -38 3
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 183787 None 0 Human Functional pEC50 = 6.3 6.3 -38 3
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 192963 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192963 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192963 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -33 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -33 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -33 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -33 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -33 3
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 138432 None 0 Human Functional pEC50 = 6.3 6.3 -33 3
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 12564 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
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 12564 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
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 12564 None 0 Human Functional pEC50 = 6.3 6.3 -4 3
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
168941519 195345 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 231 1 1 2 2.4 CN1CCC=C(c2n[nH]c3cc(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
CHEMBL5401711 195345 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 231 1 1 2 2.4 CN1CCC=C(c2n[nH]c3cc(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
11313985 91117 None 0 Human Functional pEC50 = 7.3 7.3 -15 3
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 91117 None 0 Human Functional pEC50 = 7.3 7.3 -15 3
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 216554 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 121857 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 121857 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 216554 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138435 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 138435 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 138435 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 138435 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 138435 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 138435 None 0 Human Functional pEC50 = 6.3 6.3 -19 3
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 114367 None 31 Human Functional pEC50 = 6.3 6.3 - 1
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 114367 None 31 Human Functional pEC50 = 6.3 6.3 - 1
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 19054 None 38 Human Functional pEC50 = 8.3 8.3 - 1
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 19054 None 38 Human Functional pEC50 = 8.3 8.3 - 1
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 188711 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 188711 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 188711 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 None 45 Human Functional pEC50 = 8.2 8.2 -15 26
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 None 45 Human Functional pEC50 = 8.2 8.2 -15 26
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 None 45 Human Functional pEC50 = 8.2 8.2 -15 26
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 None 45 Human Functional pEC50 = 8.2 8.2 -15 26
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 None 19 Human Functional pEC50 = 7.3 7.3 -36 5
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 None 19 Human Functional pEC50 = 7.3 7.3 -36 5
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 None 19 Human Functional pEC50 = 7.3 7.3 -36 5
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 119906 None 24 Human Functional pEC50 = 7.3 7.3 100 2
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 119906 None 24 Human Functional pEC50 = 7.3 7.3 100 2
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 8445 None 0 Human Functional pEC50 = 6.3 6.3 -100 3
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 8445 None 0 Human Functional pEC50 = 6.3 6.3 -100 3
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 169307 None 5 Human Functional pEC50 = 6.3 6.3 -46 3
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 169307 None 5 Human Functional pEC50 = 6.3 6.3 -46 3
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 12659 None 0 Human Functional pEC50 = 6.3 6.3 -95 3
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 12659 None 0 Human Functional pEC50 = 6.3 6.3 -95 3
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 12659 None 0 Human Functional pEC50 = 6.3 6.3 -95 3
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 12469 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
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 12469 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
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 12469 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
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 193094 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 193094 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 193094 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216552 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216552 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216552 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 216552 None 0 Human Functional pEC50 = 7.3 7.3 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 169307 None 5 Human Functional pEC50 = 6.3 6.3 -46 3
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 169307 None 5 Human Functional pEC50 = 6.3 6.3 -46 3
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 138433 None 1 Human Functional pEC50 = 6.3 6.3 -20 3
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 138433 None 1 Human Functional pEC50 = 6.3 6.3 -20 3
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 138433 None 1 Human Functional pEC50 = 6.3 6.3 -20 3
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 192992 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192992 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192992 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138433 None 1 Human Functional pEC50 = 6.3 6.3 -20 3
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 138433 None 1 Human Functional pEC50 = 6.3 6.3 -20 3
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 138433 None 1 Human Functional pEC50 = 6.3 6.3 -20 3
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 137327 None 0 Human Functional pEC50 = 6.3 6.3 -36 3
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 137327 None 0 Human Functional pEC50 = 6.3 6.3 -36 3
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 12684 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 12684 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 12684 None 0 Human Functional pEC50 = 6.3 6.3 -3 3
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 192992 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192992 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192992 None 0 Human Functional pEC50 = 6.3 6.3 -2 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 56864 None 0 Human Functional pEC50 = 5.3 5.3 -138 3
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 56864 None 0 Human Functional pEC50 = 5.3 5.3 -138 3
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 193094 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201903 193094 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 332 1 3 2 4.4 Oc1cc(Cl)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222595 193094 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941548 196083 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 233 1 2 2 2.6 Clc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5416604 196083 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 233 1 2 2 2.6 Clc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
11151653 91135 None 0 Human Functional pEC50 = 7.3 7.3 -6 3
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 91135 None 0 Human Functional pEC50 = 7.3 7.3 -6 3
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 192095 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 192095 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 164501 None 0 Human Functional pEC50 = 7.3 7.3 -426 3
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 164501 None 0 Human Functional pEC50 = 7.3 7.3 -426 3
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
168941715 196900 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5434434 196900 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
168291130 193085 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201835 193085 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222548 193085 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941715 196900 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
CHEMBL5434434 196900 None 0 Human Functional pEC50 = 6.3 6.3 -8 3
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assayAgonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL 229 2 2 3 1.9 COc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00566
168291130 193085 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5201835 193085 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1cc(Br)ccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222548 193085 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193080 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193080 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193080 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193080 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193080 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193080 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 12525 None 0 Human Functional pEC50 = 6.3 6.3 -13 3
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 12525 None 0 Human Functional pEC50 = 6.3 6.3 -13 3
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 12525 None 0 Human Functional pEC50 = 6.3 6.3 -13 3
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 87344 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 87344 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 87344 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 87344 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
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 79139 None 0 Human Functional pEC50 = 7.3 7.3 -5 3
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 79139 None 0 Human Functional pEC50 = 7.3 7.3 -5 3
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 192899 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192899 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192899 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
4543677 192899 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5179287 192899 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 310 1 2 1 4.7 Cc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(C)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5221372 192899 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 202194 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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 202194 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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 12648 None 0 Human Functional pEC50 = 6.2 6.2 -64 3
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 12648 None 0 Human Functional pEC50 = 6.2 6.2 -64 3
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 12648 None 0 Human Functional pEC50 = 6.2 6.2 -64 3
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 192866 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192866 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183895 None 0 Human Functional pEC50 = 6.2 6.2 -22 2
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 183895 None 0 Human Functional pEC50 = 6.2 6.2 -22 2
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 183895 None 0 Human Functional pEC50 = 6.2 6.2 -22 2
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 12448 None 1 Human Functional pEC50 = 6.2 6.2 -123 3
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 12448 None 1 Human Functional pEC50 = 6.2 6.2 -123 3
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 12448 None 1 Human Functional pEC50 = 6.2 6.2 -123 3
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 56815 None 0 Human Functional pEC50 = 6.2 6.2 4 3
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 56815 None 0 Human Functional pEC50 = 6.2 6.2 4 3
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 183895 None 0 Human Functional pEC50 = 6.2 6.2 -22 2
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 183895 None 0 Human Functional pEC50 = 6.2 6.2 -22 2
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 183895 None 0 Human Functional pEC50 = 6.2 6.2 -22 2
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
172466550 196777 None 0 Human Functional pEC50 = 6.2 6.2 -25 3
Agonist activity at 5-HT2A (unknown origin)Agonist activity at 5-HT2A (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
CHEMBL5432040 196777 None 0 Human Functional pEC50 = 6.2 6.2 -25 3
Agonist activity at 5-HT2A (unknown origin)Agonist activity at 5-HT2A (unknown origin)
ChEMBL 271 0 2 2 3.5 Oc1cc2c3c(c1Cl)-c1ccccc1CC3NCC2 10.1016/j.ejmech.2023.115414
168275014 192929 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192929 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192929 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 113142 None 27 Human Functional pEC50 = 8.2 8.2 - 1
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 113142 None 27 Human Functional pEC50 = 8.2 8.2 - 1
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 102549 None 0 Human Functional pEC50 = 8.2 8.2 1 9
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 102549 None 0 Human Functional pEC50 = 8.2 8.2 1 9
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 102549 None 0 Human Functional pEC50 = 8.2 8.2 1 9
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 67682 None 11 Human Functional pEC50 = 8.2 8.2 - 1
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 67682 None 11 Human Functional pEC50 = 8.2 8.2 - 1
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 102558 None 0 Human Functional pEC50 = 8.2 8.2 1 8
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 102558 None 0 Human Functional pEC50 = 8.2 8.2 1 8
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 102558 None 0 Human Functional pEC50 = 8.2 8.2 1 8
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 None 14 Human Functional pEC50 = 8.2 8.2 -2 4
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 None 14 Human Functional pEC50 = 8.2 8.2 -2 4
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 None 14 Human Functional pEC50 = 8.2 8.2 -2 4
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 None 14 Human Functional pEC50 = 8.2 8.2 -2 4
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 None 14 Human Functional pEC50 = 8.2 8.2 -2 4
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 None 14 Human Functional pEC50 = 8.2 8.2 -2 4
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 190088 None 1 Human Functional pEC50 = 8.2 8.2 - 1
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 190088 None 1 Human Functional pEC50 = 8.2 8.2 - 1
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
172467300 196796 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptorAgonist activity at human 5HT2A receptor
ChEMBL 251 2 1 2 3.1 CC1(C)Cc2cc(Cl)cc([C@H]3C[C@H]3CN)c2O1 10.1016/j.bmcl.2024.129654
CHEMBL5432430 196796 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptorAgonist activity at human 5HT2A receptor
ChEMBL 251 2 1 2 3.1 CC1(C)Cc2cc(Cl)cc([C@H]3C[C@H]3CN)c2O1 10.1016/j.bmcl.2024.129654
18735313 207392 None 1 Human Functional pEC50 = 6.2 6.2 -93 3
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 207392 None 1 Human Functional pEC50 = 6.2 6.2 -93 3
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 192929 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192929 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192929 None 0 Human Functional pEC50 = 6.2 6.2 -3 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 89104 None 0 Human Functional pEC50 = 6.2 6.2 -141 3
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 89104 None 0 Human Functional pEC50 = 6.2 6.2 -141 3
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 89104 None 0 Human Functional pEC50 = 6.2 6.2 -141 3
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 89146 None 0 Human Functional pEC50 = 6.2 6.2 -35 3
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 89146 None 0 Human Functional pEC50 = 6.2 6.2 -35 3
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 89146 None 0 Human Functional pEC50 = 6.2 6.2 -35 3
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 63337 None 2 Human Functional pEC50 = 7.2 7.2 -30 3
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 63337 None 2 Human Functional pEC50 = 7.2 7.2 -30 3
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
168941678 195526 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 242 2 1 2 2.9 COc1cccc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5405349 195526 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 242 2 1 2 2.9 COc1cccc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
44572806 12658 None 0 Human Functional pEC50 = 6.2 6.2 -38 3
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 12658 None 0 Human Functional pEC50 = 6.2 6.2 -38 3
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 12658 None 0 Human Functional pEC50 = 6.2 6.2 -38 3
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 None 24 Human Functional pEC50 = 6.2 6.2 -17 11
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 None 24 Human Functional pEC50 = 6.2 6.2 -17 11
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 None 24 Human Functional pEC50 = 6.2 6.2 -17 11
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 None 24 Human Functional pEC50 = 6.2 6.2 -17 11
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 None 24 Human Functional pEC50 = 6.2 6.2 -17 11
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 183741 None 0 Human Functional pEC50 = 6.2 6.2 -14 3
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 183741 None 0 Human Functional pEC50 = 6.2 6.2 -14 3
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 183741 None 0 Human Functional pEC50 = 6.2 6.2 -14 3
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 207581 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
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 207581 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
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 89105 None 0 Human Functional pEC50 = 7.2 7.2 -17 3
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 89105 None 0 Human Functional pEC50 = 7.2 7.2 -17 3
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 89105 None 0 Human Functional pEC50 = 7.2 7.2 -17 3
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 56865 None 0 Human Functional pEC50 = 7.2 7.2 3 3
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 56865 None 0 Human Functional pEC50 = 7.2 7.2 3 3
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 62625 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
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 62625 None 0 Human Functional pEC50 = 7.2 7.2 -20 3
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 None 45 Human Functional pEC50 = 7.2 7.2 -4 6
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 None 45 Human Functional pEC50 = 7.2 7.2 -4 6
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 None 45 Human Functional pEC50 = 7.2 7.2 -4 6
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 None 45 Human Functional pEC50 = 7.2 7.2 -4 6
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 64658 None 0 Human Functional pEC50 = 7.2 7.2 -7 3
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 64658 None 0 Human Functional pEC50 = 7.2 7.2 -7 3
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 122838 None 0 Human Functional pEC50 = 7.2 7.2 -10 3
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 122838 None 0 Human Functional pEC50 = 7.2 7.2 -10 3
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 202358 None 0 Human Functional pEC50 = 6.2 6.2 -67 3
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 202358 None 0 Human Functional pEC50 = 6.2 6.2 -67 3
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 183741 None 0 Human Functional pEC50 = 6.2 6.2 -14 3
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 183741 None 0 Human Functional pEC50 = 6.2 6.2 -14 3
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 183741 None 0 Human Functional pEC50 = 6.2 6.2 -14 3
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 190232 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 190232 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 72086 None 24 Human Functional pEC50 = 6.2 6.2 -21 3
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 72086 None 24 Human Functional pEC50 = 6.2 6.2 -21 3
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 91128 None 0 Human Functional pEC50 = 7.2 7.2 -12 2
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 91128 None 0 Human Functional pEC50 = 7.2 7.2 -12 2
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 193016 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193016 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193016 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193016 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193016 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193016 None 0 Human Functional pEC50 = 7.2 7.2 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
172460365 197485 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assayAgonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assay
ChEMBL 279 0 1 3 3.3 Clc1cc2nc3c(nc2cc1Cl)[C@@H]1CCC(C3)N1 10.1021/acs.jmedchem.3c01059
CHEMBL5418999 197485 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assayAgonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assay
ChEMBL 279 0 1 3 3.3 Clc1cc2nc3c(nc2cc1Cl)[C@@H]1CCC(C3)N1 10.1021/acs.jmedchem.3c01059
CHEMBL5499631 197485 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assayAgonist activity at 5-HT2A receptor in HEK293 cells assessed as calcium mobilisation by Fluo-4 dye based assay
ChEMBL 279 0 1 3 3.3 Clc1cc2nc3c(nc2cc1Cl)[C@@H]1CCC(C3)N1 10.1021/acs.jmedchem.3c01059
143111395 192924 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192924 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192924 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138436 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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 138436 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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 138436 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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 192924 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192924 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192924 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 56819 None 0 Human Functional pEC50 = 6.2 6.2 -128 3
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 56819 None 0 Human Functional pEC50 = 6.2 6.2 -128 3
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 200283 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
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 200283 None 0 Human Functional pEC50 = 7.2 7.2 -2 3
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
168941537 196049 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 240 2 2 1 3.7 CC(C)c1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5415797 196049 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 240 2 2 1 3.7 CC(C)c1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
122442300 138436 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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 138436 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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 138436 None 0 Human Functional pEC50 = 6.2 6.2 -4 3
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
168941653 196860 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 264 1 1 1 3.7 CN1CCC=C(c2c[nH]c3c(Cl)c(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
CHEMBL5433583 196860 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 264 1 1 1 3.7 CN1CCC=C(c2c[nH]c3c(Cl)c(F)ccc23)C1 10.1021/acsmedchemlett.3c00444
44572751 12503 None 0 Human Functional pEC50 = 7.2 7.2 -87 3
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 12503 None 0 Human Functional pEC50 = 7.2 7.2 -87 3
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 12503 None 0 Human Functional pEC50 = 7.2 7.2 -87 3
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 138438 None 0 Human Functional pEC50 = 7.2 7.2 -13 3
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 138438 None 0 Human Functional pEC50 = 7.2 7.2 -13 3
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 138438 None 0 Human Functional pEC50 = 7.2 7.2 -13 3
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 61474 None 27 Human Functional pEC50 = 7.2 7.2 -6 9
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 61474 None 27 Human Functional pEC50 = 7.2 7.2 -6 9
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 138438 None 0 Human Functional pEC50 = 7.2 7.2 -13 3
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 138438 None 0 Human Functional pEC50 = 7.2 7.2 -13 3
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 138438 None 0 Human Functional pEC50 = 7.2 7.2 -13 3
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
168941564 195265 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5399727 195265 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 217 1 2 2 2.1 Fc1ccc2[nH]nc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
72197311 102546 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 102546 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 102546 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 120730 None 0 Human Functional pEC50 = 6.2 6.2 -4 2
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 120730 None 0 Human Functional pEC50 = 6.2 6.2 -4 2
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 120730 None 0 Human Functional pEC50 = 6.2 6.2 -4 2
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 217086 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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
168941463 196635 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5428466 196635 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
168941766 197177 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 251 1 2 2 2.7 Fc1ccc(Cl)c2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5440436 197177 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 251 1 2 2 2.7 Fc1ccc(Cl)c2[nH]nc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
1355 2011 None 45 Human Functional pEC50 = 8.1 8.1 -4 6
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 None 45 Human Functional pEC50 = 8.1 8.1 -4 6
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 None 45 Human Functional pEC50 = 8.1 8.1 -4 6
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 None 45 Human Functional pEC50 = 8.1 8.1 -4 6
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
1043 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
149 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
8223 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
8223.0 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
CHEMBL442 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
DB00696 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
1150 3878 None 72 Human Functional pEC50 = 8.1 8.1 41 3
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 None 72 Human Functional pEC50 = 8.1 8.1 41 3
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 None 72 Human Functional pEC50 = 8.1 8.1 41 3
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 None 72 Human Functional pEC50 = 8.1 8.1 41 3
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 None 45 Human Functional pEC50 = 8.1 8.1 -15 26
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 None 45 Human Functional pEC50 = 8.1 8.1 -15 26
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 None 45 Human Functional pEC50 = 8.1 8.1 -15 26
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 None 45 Human Functional pEC50 = 8.1 8.1 -15 26
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
1043 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
149 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
8223 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
8223.0 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
CHEMBL442 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
DB00696 1582 None 6 Human Functional pEC50 = 8.1 8.1 -54 22
Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assayAgonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay
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 10.1021/acsmedchemlett.4c00058
46228437 202440 None 1 Human Functional pEC50 = 7.2 7.2 -6 3
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 202440 None 1 Human Functional pEC50 = 7.2 7.2 -6 3
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 None 45 Human Functional pEC50 = 7.2 7.2 -15 26
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 None 45 Human Functional pEC50 = 7.2 7.2 -15 26
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 None 45 Human Functional pEC50 = 7.2 7.2 -15 26
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 None 45 Human Functional pEC50 = 7.2 7.2 -15 26
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 201785 None 0 Human Functional pEC50 = 7.2 7.2 -34 4
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 201785 None 0 Human Functional pEC50 = 7.2 7.2 -34 4
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 91120 None 0 Human Functional pEC50 = 6.2 6.2 -19 2
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 91120 None 0 Human Functional pEC50 = 6.2 6.2 -19 2
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
168941728 197186 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 228 2 2 2 2.6 COc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5440705 197186 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 228 2 2 2 2.6 COc1cccc2[nH]cc(C3=CCCNC3)c12 10.1021/acsmedchemlett.3c00444
168 3982 None 15 Human Functional pEC50 = 6.1 6.1 -66 5
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 None 15 Human Functional pEC50 = 6.1 6.1 -66 5
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 None 15 Human Functional pEC50 = 6.1 6.1 -66 5
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 193092 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 193092 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 193092 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 122838 None 0 Human Functional pEC50 = 7.1 7.1 -10 3
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 122838 None 0 Human Functional pEC50 = 7.1 7.1 -10 3
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 193092 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5201470 193092 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 298 1 4 3 3.0 Oc1ccc(O)c(C2NCCc3c2[nH]c2ccc(F)cc32)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5222574 193092 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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
168941538 195747 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 243 2 1 3 2.3 COc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5410020 195747 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assayAgonist activity at 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with RLuc-fused Galphaq/GFP2/Gy9/Gbeta3 assessed as Gaq hetero trimeric G protein activation incubated for 30 mins using coelenterazine 400a as a substrate by BRET assay
ChEMBL 243 2 1 3 2.3 COc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
4305260 191134 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 191134 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 191134 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 191134 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 12551 None 0 Human Functional pEC50 = 6.1 6.1 -208 3
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 12551 None 0 Human Functional pEC50 = 6.1 6.1 -208 3
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 12551 None 0 Human Functional pEC50 = 6.1 6.1 -208 3
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
168941537 196049 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 240 2 2 1 3.7 CC(C)c1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5415797 196049 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 240 2 2 1 3.7 CC(C)c1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
168941538 195747 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 243 2 1 3 2.3 COc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5410020 195747 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 243 2 1 3 2.3 COc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
168286640 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194223 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222252 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5194223 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 376 1 3 2 4.5 Oc1c(Br)cccc1C1NCCc2c1[nH]c1ccc(Cl)cc21 10.1021/acsmedchemlett.1c00694
CHEMBL5222252 193037 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 183769 None 0 Human Functional pEC50 = 6.1 6.1 -37 3
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 183769 None 0 Human Functional pEC50 = 6.1 6.1 -37 3
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 183769 None 0 Human Functional pEC50 = 6.1 6.1 -37 3
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 183769 None 0 Human Functional pEC50 = 6.1 6.1 -37 3
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 183769 None 0 Human Functional pEC50 = 6.1 6.1 -37 3
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 183769 None 0 Human Functional pEC50 = 6.1 6.1 -37 3
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 None 45 Human Functional pEC50 = 7.1 7.1 -4 6
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 None 45 Human Functional pEC50 = 7.1 7.1 -4 6
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 None 45 Human Functional pEC50 = 7.1 7.1 -4 6
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 None 45 Human Functional pEC50 = 7.1 7.1 -4 6
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 114365 None 15 Human Functional pEC50 = 7.1 7.1 - 1
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 114365 None 15 Human Functional pEC50 = 7.1 7.1 - 1
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 187737 None 28 Human Functional pEC50 = 7.1 7.1 -95 6
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
CHEMBL4743049 187737 None 28 Human Functional pEC50 = 7.1 7.1 -95 6
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 187737 None 28 Human Functional pEC50 = 7.1 7.1 -95 6
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 183791 None 0 Human Functional pEC50 = 6.1 6.1 -28 3
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 183791 None 0 Human Functional pEC50 = 6.1 6.1 -28 3
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 183791 None 0 Human Functional pEC50 = 6.1 6.1 -28 3
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 183791 None 0 Human Functional pEC50 = 6.1 6.1 -28 3
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 183791 None 0 Human Functional pEC50 = 6.1 6.1 -28 3
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 183791 None 0 Human Functional pEC50 = 6.1 6.1 -28 3
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 187737 None 28 Human Functional pEC50 = 7.1 7.1 -95 6
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
CHEMBL4743049 187737 None 28 Human Functional pEC50 = 7.1 7.1 -95 6
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 187737 None 28 Human Functional pEC50 = 7.1 7.1 -95 6
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 207419 None 0 Human Functional pEC50 = 7.1 7.1 -18 3
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 207419 None 0 Human Functional pEC50 = 7.1 7.1 -18 3
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 56868 None 0 Human Functional pEC50 = 6.1 6.1 -91 3
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 56868 None 0 Human Functional pEC50 = 6.1 6.1 -91 3
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
168941703 196195 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 227 1 1 2 2.6 Cc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
CHEMBL5418595 196195 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 227 1 1 2 2.6 Cc1ccnc2[nH]cc(C3=CCCN(C)C3)c12 10.1021/acsmedchemlett.3c00444
122442251 138447 None 0 Human Functional pEC50 = 6.1 6.1 -47 3
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 138447 None 0 Human Functional pEC50 = 6.1 6.1 -47 3
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 138447 None 0 Human Functional pEC50 = 6.1 6.1 -47 3
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 102550 None 0 Human Functional pEC50 = 7.1 7.1 -4 7
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 102550 None 0 Human Functional pEC50 = 7.1 7.1 -4 7
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 102550 None 0 Human Functional pEC50 = 7.1 7.1 -4 7
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 12687 None 0 Human Functional pEC50 = 6.1 6.1 -6 3
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 12687 None 0 Human Functional pEC50 = 6.1 6.1 -6 3
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 12687 None 0 Human Functional pEC50 = 6.1 6.1 -6 3
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 193084 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193084 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193084 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193084 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193084 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193084 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138447 None 0 Human Functional pEC50 = 6.1 6.1 -47 3
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 138447 None 0 Human Functional pEC50 = 6.1 6.1 -47 3
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 138447 None 0 Human Functional pEC50 = 6.1 6.1 -47 3
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 56818 None 0 Human Functional pEC50 = 5.1 5.1 -436 3
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 56818 None 0 Human Functional pEC50 = 5.1 5.1 -436 3
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 83476 None 0 Human Functional pEC50 = 7.1 7.1 -3 3
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 83476 None 0 Human Functional pEC50 = 7.1 7.1 -3 3
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
168941463 196635 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
CHEMBL5428466 196635 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assayAgonist activity at RLuc-fused 5-HT2A (unknown origin) expressed in HEK293T cells co-transfected with mVenus-fused beta arrestin-2/GRK2 assessed as beta arrestin-2 recruitment incubated for 30 mins using coelenterazine h as a substrate by BRET assay
ChEMBL 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCCNC3)c2c1 10.1021/acsmedchemlett.3c00444
168277089 192948 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192948 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192948 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192948 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192948 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192948 None 0 Human Functional pEC50 = 7.1 7.1 1 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 87340 None 1 Human Functional pEC50 = 5.1 5.1 -2 2
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 87340 None 1 Human Functional pEC50 = 5.1 5.1 -2 2
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 130467 None 3 Human Functional pEC50 = 6.1 6.1 -38 3
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 130467 None 3 Human Functional pEC50 = 6.1 6.1 -38 3
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 138448 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 138448 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 138448 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 87340 None 1 Human Functional pEC50 = 5.1 5.1 -2 2
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 87340 None 1 Human Functional pEC50 = 5.1 5.1 -2 2
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 192316 None 0 Human Functional pEC50 = 5.1 5.1 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192316 None 0 Human Functional pEC50 = 5.1 5.1 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 138448 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 138448 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 138448 None 0 Human Functional pEC50 = 6.1 6.1 -9 3
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 190079 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 190079 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 178231 None 20 Human Functional pEC50 = 8.1 8.1 5 2
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 178231 None 20 Human Functional pEC50 = 8.1 8.1 5 2
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 190079 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 190079 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 178231 None 20 Human Functional pEC50 = 8.1 8.1 5 2
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 178231 None 20 Human Functional pEC50 = 8.1 8.1 5 2
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 210385 None 21 Human Functional pEC50 = 8.1 8.1 18 2
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 210385 None 21 Human Functional pEC50 = 8.1 8.1 18 2
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 190982 None 8 Human Functional pEC50 = 8.1 8.1 14 2
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 190982 None 8 Human Functional pEC50 = 8.1 8.1 14 2
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 64130 None 0 Human Functional pEC50 = 7.1 7.1 -15 3
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 64130 None 0 Human Functional pEC50 = 7.1 7.1 -15 3
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 64202 None 0 Human Functional pEC50 = 7.1 7.1 -26 3
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 64202 None 0 Human Functional pEC50 = 7.1 7.1 -26 3
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 64658 None 0 Human Functional pEC50 = 7.1 7.1 -7 3
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 64658 None 0 Human Functional pEC50 = 7.1 7.1 -7 3
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 192106 None 0 Human Functional pEC50 = 6.1 6.1 8 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192106 None 0 Human Functional pEC50 = 6.1 6.1 8 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192316 None 0 Human Functional pEC50 = 5.1 5.1 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 192316 None 0 Human Functional pEC50 = 5.1 5.1 -6 2
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in 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 193155 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5208864 193155 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assayAgonist activity at human 5HT2A receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL 342 3 2 3 4.1 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222941 193155 None 0 Human Functional pEC50 =